Strategies to Address Low Drug Solubility in Discovery and Development
Tóm tắt
Từ khóa
Tài liệu tham khảo
Aakeröy, 2005, Building co-crystals with molecular sense and supramolecular sensibility, Cryst Eng Comm, 7, 439, 10.1039/b505883j
Aakeröy CB Schultheiss N (2007) Assembly of molecular solids via non-covalent interactions, in Making Crystals by Design: Methods, Techniques and Applications ( Braga D Grepioni F eds) pp 209–240, Wiley-VCH, Weinheim, Germany.
Abdalla, 2008, A new self-emulsifying drug delivery system (SEDDS) for poorly soluble drugs: characterization, dissolution, in vitro digestion and incorporation into solid pellets, Eur J Pharm Sci, 35, 457, 10.1016/j.ejps.2008.09.006
Abdalla, 2009, ESR studies on the influence of physiological dissolution and digestion media on the lipid phase characteristics of SEDDS and SEDDS pellets, Int J Pharm, 367, 29, 10.1016/j.ijpharm.2008.09.014
Abu-Diak, 2011, An investigation into the dissolution properties of celecoxib melt extrudates: understanding the role of polymer type and concentration in stabilizing supersaturated drug concentrations, Mol Pharm, 8, 1362, 10.1021/mp200157b
Adam, 2000, Factors influencing capping and cracking of mefenamic acid tablets, Drug Dev Ind Pharm, 26, 489, 10.1081/DDC-100101259
Adrjanowicz, 2010, Dielectric relaxation studies and dissolution behavior of amorphous verapamil hydrochloride, J Pharm Sci, 99, 828, 10.1002/jps.21877
Adrjanowicz, 2010, Determining the structural relaxation times deep in the glassy state of the pharmaceutical telmisartan, J Phys Condens Matter, 22, 125902, 10.1088/0953-8984/22/12/125902
Agarwal, 2009, Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS), Int J Pharm, 366, 44, 10.1016/j.ijpharm.2008.08.046
Agharkar, 1976, Enhancement of solubility of drug salts by hydrophilic counterions: properties of organic salts of an antimalarial drug, J Pharm Sci, 65, 747, 10.1002/jps.2600650533
Agoram B Sagawa K Shanker RM Singh SK (2010) Biopharmaceutics of NCEs and NBEs, in Pharmaceutical Dosage Forms: Parenteral Medications ( Nema S Ludwig JD eds) Informa Healthcare, New York.
Agüeros, 2010, Increased oral bioavailability of paclitaxel by its encapsulation through complex formation with cyclodextrins in poly(anhydride) nanoparticles, J Control Release, 145, 2, 10.1016/j.jconrel.2010.03.012
Aguiar, 1967, Effect of polymorphism on the absorption of chloramphenicol from chloramphenicol palmitate, J Pharm Sci, 56, 847, 10.1002/jps.2600560712
Aguiar, 1969, Dissolution behavior of polymorphs of chloramphenicol palmitate and mefenamic acid, J Pharm Sci, 58, 983, 10.1002/jps.2600580817
Ahmed, 2012, Nanoemulsion- and emulsion-based delivery systems for curcumin: encapsulation and release properties, Food Chem, 132, 799, 10.1016/j.foodchem.2011.11.039
Ahmed, 2001, Comparison of impact of the different hydrophilic carriers on the properties of piperazine-containing drug, Eur J Pharm Biopharm, 51, 221, 10.1016/S0939-6411(01)00128-X
Ainouz, 2009, Modeling and prediction of cocrystal phase diagrams, Int J Pharm, 374, 82, 10.1016/j.ijpharm.2009.03.016
Alie, 2004, Dielectric study of the molecular mobility and the isothermal crystallization kinetics of an amorphous pharmaceutical drug substance, J Pharm Sci, 93, 218, 10.1002/jps.10520
Allen, 1978, Dissolution rates of hydrocortisone and prednisone utilizing sugar solid dispersion systems in tablet form, J Pharm Sci, 67, 979, 10.1002/jps.2600670729
Al-Marzouqi, 2006, Phase solubility and inclusion complex of itraconazole with beta-cyclodextrin using supercritical carbon dioxide, J Pharm Sci, 95, 292, 10.1002/jps.20535
Alonzo, 2011, Dissolution and precipitation behavior of amorphous solid dispersions, J Pharm Sci, 100, 3316, 10.1002/jps.22579
Alvarez-Núñez, 2000, Relationship between polysorbate 80 solubilization descriptors and octanol-water partition coefficients of drugs, Int J Pharm, 200, 217, 10.1016/S0378-5173(00)00386-0
Ambrogi, 2007, Improvement of dissolution rate of piroxicam by inclusion into MCM-41 mesoporous silicate, Eur J Pharm Sci, 32, 216, 10.1016/j.ejps.2007.07.005
Ambrogi, 2012, MCM-41 for furosemide dissolution improvement, Microporous Mesoporous Mater, 147, 343, 10.1016/j.micromeso.2011.07.007
Amin, 2006, In vitro hemolysis: guidance for the pharmaceutical scientist, J Pharm Sci, 95, 1173, 10.1002/jps.20627
Anby, 2012, Lipid digestion as a trigger for supersaturation: evaluation of the impact of supersaturation stabilization on the in vitro and in vivo performance of self-emulsifying drug delivery systems, Mol Pharm, 9, 2063, 10.1021/mp300164u
Anderberg, 1988, Physicochemical aspects of drug release. 7. The effect of surfactant concentration and drug particle-size on solubility and dissolution rate of felodipine, a sparingly soluble drug, Int J Pharm, 47, 67, 10.1016/0378-5173(88)90216-5
Anderson, 1985, Predictive relationships in the water solubility of salts of a nonsteroidal anti-inflammatory drug, J Pharm Sci, 74, 815, 10.1002/jps.2600740803
Andronis, 1997, Molecular mobility of supercooled amorphous indomethacin, determined by dynamic mechanical analysis, Pharm Res, 14, 410, 10.1023/A:1012026911459
Andronis, 1998, The molecular mobility of supercooled amorphous indomethacin as a function of temperature and relative humidity, Pharm Res, 15, 835, 10.1023/A:1011960112116
Angell CA (2011) Heat capacity and entropy functions in strong and fragile glass-formers, relative to those of disordering crystalline materials, in Hot Topics in Thermal Analysis and Calorimetry #8: Glassy, Amorphous and Nano-Crystalline Materials: Thermal Physics, Analysis, Structure and Properties ( Sestak J Mares JJ Hubik P eds) pp 21–40, Springer, New York.
Angell, 1980, Heat-capacity changes in glass-forming aqueous-solutions and the glass-transition in vitreous water, J Phys Chem, 84, 268, 10.1021/j100440a009
Angell, 2003, Potential energy, relaxation, vibrational dynamics and the boson peak, of hyperquenched glasses, J Phys Condens Matter, 15, S1051, 10.1088/0953-8984/15/11/327
Antlsperger G Schmid G (1996) Toxicological comparison of cyclodextrins, in Proceedings of the 8th International Symposium on Cyclodextrins ( Szejtli J Szente L eds) Kluwer Academic Publishers; 1996 March 31 and April 2; Budapest, Hungary.
Aramwit, 2006, In vitro plasma compatibility study of a nanosuspension formulation, PDA J Pharm Sci Technol, 60, 211
Arias, 1995, Influence of the preparation method of solid dispersions on their dissolution rate: study of triamterene-D-mannitol system, Int J Pharm, 123, 25, 10.1016/0378-5173(95)00026-F
Arima, 2001, Contribution of P-glycoprotein to the enhancing effects of dimethyl-beta-cyclodextrin on oral bioavailability of tacrolimus, J Pharmacol Exp Ther, 297, 547
Arimori, 1987, Effects of beta- and gamma-cyclodextrins on the pharmacokinetic behavior of prednisolone after intravenous and intramuscular administrations to rabbits, J Pharmacobiodyn, 10, 390, 10.1248/bpb1978.10.390
Armstrong, 1996, Effect of cosolvents and cosolutes upon aggregation transitions in aqueous solutions of the poloxamer F87 (poloxamer P237): a high sensitivity differential scanning calorimetry study, J Phys Chem, 100, 1738, 10.1021/jp951390s
Arnarson, 1982, Effects of structural variations of non-ionic surfactants on micellar properties and solubilization: variation of oxyethylene content on properties of C22 monoethers, J Pharm Pharmacol, 34, 87, 10.1111/j.2042-7158.1982.tb04191.x
Arnesjö, 1971, The activation, purification and properties of rat pancreatic juice phospholipase A 2, Acta Chem Scand, 25, 577, 10.3891/acta.chem.scand.25-0577
Arora KK Zaworotko MJ (2009) Pharmaceutical co-crystals: a new opportunity in pharmaceutical science for a long-known but little-studied class of compounds, in Polymorphism in Pharmaceutical Solids ( Brittain HG ed) pp 282–317, Informa Healthcare, New York.
Aso, 2000, Relationship between the crystallization rates of amorphous nifedipine, phenobarbital, and flopropione, and their molecular mobility as measured by their enthalpy relaxation and (1)H NMR relaxation times, J Pharm Sci, 89, 408, 10.1002/(SICI)1520-6017(200003)89:3<408::AID-JPS11>3.0.CO;2-#
Attwood D Florence AT (1983) Surfactant Systems: Their Chemistry, Pharmacy and Biology, Chapman and Hall, London.
Augustijns, 2012, Supersaturating drug delivery systems: fast is not necessarily good enough, J Pharm Sci, 101, 7, 10.1002/jps.22750
Avis KE Lachman L Lieberman HA (1986) Pharmaceutical Dosage Forms: Parenteral Medications, Marcel Dekker, New York.
Badens, 2009, Comparison of solid dispersions produced by supercritical antisolvent and spray-freezing technologies, Int J Pharm, 377, 25, 10.1016/j.ijpharm.2009.04.047
Badrinarayanan, 2007, The glass transition temperature versus the fictive temperature, J Non-Cryst Solids, 353, 2603, 10.1016/j.jnoncrysol.2007.04.025
Bahadur, 1992, Effect of potassium fluoride on the micellar behavior of pluronic F-68 in aqueous-solution, Langmuir, 8, 1903, 10.1021/la00044a005
Bahl, 2006, Amorphization of indomethacin by co-grinding with neusilin US2: amorphization kinetics, physical stability and mechanism, Pharm Res, 23, 2317, 10.1007/s11095-006-9062-x
Bahrami, 2007, Production of micro- and nano-composite particles by supercritical carbon dioxide, J Supercrit Fluids, 40, 263, 10.1016/j.supflu.2006.05.006
Baird, 2011, Evaluation and modeling of the eutectic composition of various drug-polyethylene glycol solid dispersions, Pharm Dev Technol, 16, 201, 10.3109/10837450903584936
Baird, 2012, Evaluation of amorphous solid dispersion properties using thermal analysis techniques, Adv Drug Deliv Rev, 64, 396, 10.1016/j.addr.2011.07.009
Baird, 2010, A classification system to assess the crystallization tendency of organic molecules from undercooled melts, J Pharm Sci, 99, 3787, 10.1002/jps.22197
Bak, 2008, The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics, J Pharm Sci, 97, 3942, 10.1002/jps.21280
Balbach, 2004, Pharmaceutical evaluation of early development candidates “the 100 mg-approach.”, Int J Pharm, 275, 1, 10.1016/j.ijpharm.2004.01.034
Banerjee, 2005, Saccharin salts of active pharmaceutical ingredients, their crystal structures, and increased water solubilities, Cryst Growth Des, 5, 2299, 10.1021/cg050125l
Bansal, 2007, Molecular and thermodynamic aspects of solubility advantage from solid dispersions, Mol Pharm, 4, 794, 10.1021/mp7000796
Barry, 1976, Solubilization of hydrocortisone, dexamethasone, testosterone and progesterone by long-chain polyoxyethylene surfactants, J Pharm Pharmacol, 28, 210, 10.1111/j.2042-7158.1976.tb04133.x
Barta, 2008, Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers, Mol Pharm, 5, 863, 10.1021/mp800050q
Bartolini, 1981, Eseroline: a new antinociceptive agent derived from physostigmine with opiate receptor agonist properties: experimental in vivo and in vitro studies on cats and rodents, Neurosci Lett, 25, 179, 10.1016/0304-3940(81)90328-1
Bartolomei, 2006, Physico-chemical characterisation and intrinsic dissolution studies of a new hydrate form of diclofenac sodium: comparison with anhydrous form, J Pharm Biomed Anal, 40, 1105, 10.1016/j.jpba.2005.09.009
Bastin, 2000, Salt selection and optimisation procedures for pharmaceutical new chemical entities, Org Process Res Dev, 4, 427, 10.1021/op000018u
Becher P (1967) Micelle formation in aqueous and nonaqueous solutions, in Nonionic Surfactants ( Schick JM ed) pp 478–515, Marcel Dekker, New York.
Behrens, 1996, Comparison of cyclosporin A absorption from LCT and MCT solutions following intrajejunal administration in conscious dogs, J Pharm Sci, 85, 666, 10.1021/js9503791
Bekers, 1991, Cyclodextrins in the pharmaceutical field, Drug Dev Ind Pharm, 17, 1503, 10.3109/03639049109026630
Bergeron, 1978, Dependence of cycloamylose-substrate binding on charge, J Am Chem Soc, 100, 2878, 10.1021/ja00477a051
Beskid, 1988, Enteral, oral, and rectal absorption of ceftriaxone using glyceride enhancers, Chemotherapy, 34, 77, 10.1159/000238551
Bethune, 2009, Understanding and predicting the effect of cocrystal components and pH on cocrystal solubility, Cryst Growth Des, 9, 3976, 10.1021/cg9001187
Bettinetti, 1992, Thermal-behavior and dissolution properties of naproxen in combinations with chemically modified beta-cyclodextrins, Drug Dev Ind Pharm, 18, 39, 10.3109/03639049209043682
Bettinetti, 1991, Carbon-13 nuclear magnetic resonance study of naproxen interaction with cyclodextrins in solution, J Pharm Sci, 80, 1162, 10.1002/jps.2600801214
Bevernage, 2011, Excipient-mediated supersaturation stabilization in human intestinal fluids, Mol Pharm, 8, 564, 10.1021/mp100377m
Bhakay, 2011, Novel aspects of wet milling for the production of microsuspensions and nanosuspensions of poorly water-soluble drugs, Drug Dev Ind Pharm, 37, 963, 10.3109/03639045.2010.551775
Bharatiya, 2007, Aggregation and clouding behavior of aqueous solution of EO-PO block copolymer in presence of n-alkanols, Eur Polym J, 43, 1883, 10.1016/j.eurpolymj.2007.02.010
Bhat, 2008, Solubilization capabilities of some cationic, anionic, and nonionic surfactants toward the poorly water-soluble antibiotic drug erythromycin, J Chem Eng Data, 53, 1271, 10.1021/je700659g
Bhat, 2006, Use of novel cationic bile salts in cholesterol crystallization and solubilization in vitro, Biochim Biophys Acta, 1760, 1489, 10.1016/j.bbagen.2006.06.013
Bhattacharya, 2009, Local mobility in amorphous pharmaceuticals—characterization and implications on stability, J Pharm Sci, 98, 2935, 10.1002/jps.21728
Bhugra, 2008, Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state, J Pharm Sci, 97, 1329, 10.1002/jps.21138
Biradha, 2011, Recent developments in crystal engineering, Cryst Growth Des, 11, 875, 10.1021/cg101241x
Bittner, 2002, Improvement of the bioavailability of colchicine in rats by co-administration of D-alpha-tocopherol polyethylene glycol 1000 succinate and a polyethoxylated derivative of 12-hydroxy-stearic acid, Arzneimittelforschung, 52, 684
Bittner, 2002, Intravenous administration of poorly soluble new drug entities in early drug discovery: the potential impact of formulation on pharmacokinetic parameters, Curr Opin Drug Discov Devel, 5, 59
Bitz, 1996, Influence of the preparation method on residual solvents in biodegradable microspheres, Int J Pharm, 131, 171, 10.1016/0378-5173(95)04320-9
Black, 2007, Structure, solubility, screening, and synthesis of molecular salts, J Pharm Sci, 96, 1053, 10.1002/jps.20927
Blagden, 2007, Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates, Adv Drug Deliv Rev, 59, 617, 10.1016/j.addr.2007.05.011
Bloedow, 1976, Effects of lipids on bioavailability of sulfisoxazole acetyl, dicumarol, and griseofulvin in rats, J Pharm Sci, 65, 328, 10.1002/jps.2600650304
Bogardus, 1979, Solubility of doxycycline in aqueous solution, J Pharm Sci, 68, 188, 10.1002/jps.2600680218
Bogman, 2005, P-glycoprotein and surfactants: effect on intestinal talinolol absorption, Clin Pharmacol Ther, 77, 24, 10.1016/j.clpt.2004.09.001
Bom, 2002, A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host, Angew Chem Int Ed Engl, 41, 266
Bonini, 2006, Self-assembly of beta-cyclodextrin in water. Part 1. Cryo-TEM and dynamic and static light scattering, Langmuir, 22, 1478, 10.1021/la052878f
Bouqet MP Wagner DR (2012) Injectable formulations of poorly water-soluble drugs, in Formulating Poorly Water-Soluble Drugs ( Williams RO Watts AB Miller DA eds) pp 209–242, Springer, New York.
Boyd, 2008, Past and future evolution in colloidal drug delivery systems, Expert Opin Drug Deliv, 5, 69, 10.1517/17425247.5.1.69
Boyd BJ (2012) LIPIDS: Towards an understanding of nanostructures formed during digestion, and their impact on drug delivery and absorption. Am Pharmaceutical Rev 15:58.
Boyd, 2009, Nonlamellar liquid crystalline nanostructured particles: advances in materials and structure determination, J Liposome Res, 19, 12, 10.1080/08982100802691983
Branham, 2012, Preparation and solid-state characterization of ball milled saquinavir mesylate for solubility enhancement, Eur J Pharm Biopharm, 80, 194, 10.1016/j.ejpb.2011.08.005
Bras AR Dionisio M Correia NT (2008) Molecular motions in amorphous pharmaceuticals, in Complex Systems ( Tokuyama M Oppenheim I Nishiyama H eds) pp 91–96; AIP Conference Proceedings; 2007 September 25–28; Sendai Japan.
Bras, 2011, Amorphous ibuprofen confined in nanostructured silica materials: a dynamical approach, J Phys Chem C, 115, 4616, 10.1021/jp107631m
Bravo González, 2004, In vitro investigation on the impact of the surface-active excipients remophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam, Biopharm Drug Dispos, 25, 37, 10.1002/bdd.383
Brazeau, 2011, Effect of particle size of parenteral suspensions on in vitro muscle damage, Pharm Dev Technol, 16, 591, 10.3109/10837450.2010.542161
Breitenbach, 1999, Confocal Raman-spectroscopy: analytical approach to solid dispersions and mapping of drugs, Pharm Res, 16, 1109, 10.1023/A:1018956304595
Brewster, 1991, Development of aqueous parenteral formulations for carbamazepine through the use of modified cyclodextrins, J Pharm Sci, 80, 380, 10.1002/jps.2600800420
Brewster, 1989, The potential use of cyclodextrins in parenteral formulations, J Parenter Sci Technol, 43, 231
Brewster, 2002, A novel cyclodextrin-containing glass thermoplastic system (GTS) for formulating poorly water soluble drug candidates: preclinical and clinical results, J Incl Phenom Macrocycl Chem, 44, 35, 10.1023/A:1023076631110
Brewster, 2008, Supersaturating drug delivery systems: effect of hydrophilic cyclodextrins and other excipients on the formation and stabilization of supersaturated drug solutions, Pharmazie, 63, 217
Bristol-Myers Squibb Company (2007) Prescribing Information Taxol (pacliataxel) injection. Princeton, NJ.
Brocks, 2002, The influence of lipids on stereoselective pharmacokinetics of halofantrine: important implications in food-effect studies involving drugs that bind to lipoproteins, J Pharm Sci, 91, 1817, 10.1002/jps.10182
Broman, 2001, A comparison of alternative polymer excipients and processing methods for making solid dispersions of a poorly water soluble drug, Int J Pharm, 222, 139, 10.1016/S0378-5173(01)00709-8
Brouwers, 2009, Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability?, J Pharm Sci, 98, 2549, 10.1002/jps.21650
Bruce, 2010, The influence of heterogeneous nucleation on the surface crystallization of guaifenesin from melt extrudates containing Eudragit L10055 or Acryl-EZE, Eur J Pharm Biopharm, 75, 71, 10.1016/j.ejpb.2009.12.001
Brunner, 2000, Effect of dietary oil intake on hepatic cytochrome P450 activity in the rat, J Pharm Sci, 89, 1022, 10.1002/1520-6017(200008)89:8<1022::AID-JPS6>3.0.CO;2-O
Buggins, 2007, The effects of pharmaceutical excipients on drug disposition, Adv Drug Deliv Rev, 59, 1482, 10.1016/j.addr.2007.08.017
Bunjes, 2010, Lipid nanoparticles for the delivery of poorly water-soluble drugs, J Pharm Pharmacol, 62, 1637, 10.1111/j.2042-7158.2010.01024.x
Burcham, 1995, The effect of absorption enhancers on the oral absorption of the GP IIB/IIIA receptor antagonist, DMP 728, in rats and dogs, Pharm Res, 12, 2065, 10.1023/A:1016289200422
Buschmann, 2000, Cucurbituril and alpha- and beta-cyclodextrins as ligands for the complexation of nonionic surfactants and polyethyleneglycols in aqueous solutions, J Incl Phenom Macrocycl Chem, 37, 231, 10.1023/A:1008148831359
Butler, 2010, The developability classification system: application of biopharmaceutics concepts to formulation development, J Pharm Sci, 99, 4940, 10.1002/jps.22217
Byrn SR Stowell JG Pfeiffer R (1999) Solid State Chemistry of Drugs, SSCI Press, West Lafayette, IN.
Byrn, 2010, Accelerating proof of concept for small molecule drugs using solid-state chemistry, J Pharm Sci, 99, 3665, 10.1002/jps.22215
Cabral Marques, 1990, Studies of cyclodextrin inclusion complexes. 1. The salbutamol-cyclodextrin complex as studied by phase solubility and Dsc, Int J Pharm, 63, 259, 10.1016/0378-5173(90)90132-N
Cal K Sollohub K (2010) Spray drying technique. I: Hardware and process parameters. J Pharm Sci 586.
Caliph, 2009, Oral bioavailability assessment and intestinal lymphatic transport of Org 45697 and Org 46035, two highly lipophilic novel immunomodulator analogues, Curr Drug Deliv, 6, 359, 10.2174/156720109789000500
Caliph, 2012, Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies, J Pharmaceutical Sci, 101, 3540, 10.1002/jps.23211
Cannon BJ Shi Y Gupta P (2008) Emulsions, microemulsions, and lipid-based drug delivery systems for drug solubilization and delivery. Part I: parenteral applications, in Water-Insoluble Drug Formulation ( Rong L ed) pp 195–226, Taylor and Francis, New York.
Cannon JB (2008) Chemical and physical stability considerations for lipid-based drug formulations. Am Pharmaceutical Rev January/February:132–138.
Capaccioli, 2008, Critical issues of current research on the dynamics leading to glass transition, J Phys Chem B, 112, 16035, 10.1021/jp8057433
Cappello, 2007, Combined effect of hydroxypropyl methylcellulose and hydroxypropyl-beta-cyclodextrin on physicochemical and dissolution properties of celecoxib, J Incl Phenom Macrocycl Chem, 59, 237, 10.1007/s10847-007-9319-y
Carale, 1994, Salt effects on intramicellar interactions and micellization of nonionic surfactants in aqueous-solutions, Langmuir, 10, 109, 10.1021/la00013a016
Carlert, 2010, Predicting intestinal precipitation: a case example for a basic BCS class II drug, Pharm Res, 27, 2119, 10.1007/s11095-010-0213-8
Caron, 2010, Prediction of onset of crystallization in amorphous pharmaceutical systems: phenobarbital, nifedipine/PVP, and phenobarbital/PVP, J Pharm Sci, 99, 3887, 10.1002/jps.22232
Carstensen JT (1995) Drug Stability: Principles and Practices, Marcel Dekker, Inc., New York.
Cavallari, 2005, Thermal and fractal analysis of diclofenac/Gelucire 50/13 microparticles obtained by ultrasound-assisted atomization, J Pharm Sci, 94, 1124, 10.1002/jps.20337
Cavalli, 1999, Albumin adsorption on stealth and non-stealth solid lipid nanoparticles, STP Pharma Sci, 9, 183
Chan, 2011, Production methods for nanodrug particles using the bottom-up approach, Adv Drug Deliv Rev, 63, 406, 10.1016/j.addr.2011.03.011
Chan, 2004, FTIR spectroscopic imaging of dissolution of a solid dispersion of nifedipine in poly(ethylene glycol), Mol Pharm, 1, 331, 10.1021/mp049973m
Chan, 2004, Vitamin E formulation affects digoxin absorption by inhibiting P-glycoprotein (P-gp) in humans, Clin Pharmacol Ther, 75, 95, 10.1016/j.clpt.2003.11.364
Chan, 1998, Evaluation of a targeted prodrug strategy of enhance oral absorption of poorly water-soluble compounds, Pharm Res, 15, 1012, 10.1023/A:1011969808907
Chang, 2004, Effect of a lipoidic excipient on the absorption profile of compound UK 81252 in dogs after oral administration, J Pharm Pharm Sci, 7, 8
Charman, 1992, Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound, Pharm Res, 9, 87, 10.1023/A:1018987928936
Charman, 1993, Effect of food and a monoglyceride emulsion formulation on danazol bioavailability, J Clin Pharmacol, 33, 381, 10.1002/j.1552-4604.1993.tb04673.x
Chaubal, 2004, Application of drug delivery technologies in lead candidate selection and optimization, Drug Discov Today, 9, 603, 10.1016/S1359-6446(04)03171-X
Chauhan, 2005, Preparation and characterization of etoricoxib solid dispersions using lipid carriers by spray drying technique, AAPS PharmSciTech, 6, E405, 10.1208/pt060350
Chemburkar, 2000, Dealing with the impact of ritonavir polymorphs on the late stages of bulk drug process development, Org Process Res Dev, 4, 413, 10.1021/op000023y
Chen, 2007, Effect of injection routes on pharmacokinetics and lactone/carboxylate equilibrium of 9-nitrocamptothecin in rats, Int J Pharm, 340, 29, 10.1016/j.ijpharm.2007.03.008
Chen, 1998, Effect of hydrophobic chain length of surfactants on enthalpy-entropy compensation of micellization, J Phys Chem B, 102, 4350, 10.1021/jp9804345
Chen, 2008, Lipid excipients and delivery systems for pharmaceutical development: a regulatory perspective, Adv Drug Deliv Rev, 60, 768, 10.1016/j.addr.2007.09.010
Chen, 2011, The BCS, BDDCS, and regulatory guidances, Pharm Res, 28, 1774, 10.1007/s11095-011-0438-1
Chen, 2004, Rapid dissolution of high potency itraconazole particles produced by evaporative precipitation into aqueous solution, J Drug Delivery Sci Technol, 14, 299, 10.1016/S1773-2247(04)50051-5
Chen, 2006, Discovery pharmaceutics: challenges and opportunities, AAPS J, 8, E402, 10.1007/BF02854912
Chen, 2002, Preparation of cyclosporine A nanoparticles by evaporative precipitation into aqueous solution, Int J Pharm, 242, 3, 10.1016/S0378-5173(02)00147-3
Chen, 2004, Enhancing the bioavailability of ABT-963 using solid dispersion containing Pluronic F-68, Int J Pharm, 286, 69, 10.1016/j.ijpharm.2004.08.009
Chen, 2010, Solid solubility of antilipemic agents and micronization of gemfibrozil in supercritical carbon dioxide, J Supercrit Fluids, 52, 175, 10.1016/j.supflu.2009.12.012
Cheney, 2010, Effects of crystal form on solubility and pharmacokinetics: a crystal engineering case study of lamotrigine, Cryst Growth Des, 10, 394, 10.1021/cg901010v
Cheney, 2011, Coformer selection in pharmaceutical cocrystal development: a case study of a meloxicam aspirin cocrystal that exhibits enhanced solubility and pharmacokinetics, J Pharm Sci, 100, 2172, 10.1002/jps.22434
Cherukuvada, 2011, Nitrofurantoin-p-aminobenzoic acid cocrystal: hydration stability and dissolution rate studies, J Pharm Sci, 100, 3233, 10.1002/jps.22546
Chiang, 2009, Aqueous versus non-aqueous salt delivery strategies to enhance oral bioavailability of a mitogen-activated protein kinase-activated protein kinase (MK-2) inhibitor in rats, J Pharm Sci, 98, 248, 10.1002/jps.21425
Chiarella, 2007, Making co-crystals: the utility of ternary phase diagrams, Cryst Growth Des, 7, 1223, 10.1021/cg070218y
Chien, 1981, Long-acting parenteral drug formulations, J Parenter Sci Technol, 35, 106
Childs, 2004, Crystal engineering approach to forming cocrystals of amine hydrochlorides with organic acids: molecular complexes of fluoxetine hydrochloride with benzoic, succinic, and fumaric acids, J Am Chem Soc, 126, 13335, 10.1021/ja048114o
Childs, 2007, Cocrystals of piroxicam with carboxylic acids, Cryst Growth Des, 7, 1291, 10.1021/cg060742p
Childs, 2008, Screening strategies based on solubility and solution composition generate pharmaceutically acceptable cocrystals of carbamazepine, Cryst Eng Comm, 10, 856, 10.1039/b715396a
Childs, 2009, The reemergence of cocrystals: the crystal clear writing is on the wall introduction to virtual special issue on pharmaceutical cocrystals, Cryst Growth Des, 9, 4208, 10.1021/cg901002y
Chingunpitak, 2008, Micronization of dihydroartemisinin by rapid expansion of supercritical solutions, Drug Dev Ind Pharm, 34, 609, 10.1080/03639040701833682
Chiou, 1970, Oral absorption of griseofulvin in dogs: increased absorption via solid dispersion in polyethylene glycol 6000, J Pharm Sci, 59, 937, 10.1002/jps.2600590703
Choo, 2011, Preclinical assessment of novel BRAF inhibitors: integrating pharmacokinetic-pharmacodynamic modelling in the drug discovery process, Xenobiotica, 41, 1076, 10.3109/00498254.2011.603384
Chow, 2008, Engineering of pharmaceutical materials: an industrial perspective, J Pharm Sci, 97, 2855, 10.1002/jps.21212
Chow, 1979, A dual, concentration-dependent absorption mechanism of linoleic acid by rat jejunum in vitro, J Lipid Res, 20, 349, 10.1016/S0022-2275(20)40617-0
Chowdary, 2006, Influence of hydrophilic polymers on celecoxib complexation with hydroxypropyl beta-cyclodextrin, AAPS PharmSciTech, 7, 79, 10.1208/pt070379
Chowhan, 1978, pH-solubility profiles or organic carboxylic acids and their salts, J Pharm Sci, 67, 1257, 10.1002/jps.2600670918
Christensen, 2001, Technical optimisation of redispersible dry emulsions, Int J Pharm, 212, 195, 10.1016/S0378-5173(00)00595-0
Christiansen, 2011, Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro, Eur J Pharm Biopharm, 78, 166, 10.1016/j.ejpb.2010.12.033
Christiansen, 2010, Effects of non-ionic surfactants on in vitro triglyceride digestion and their susceptibility to digestion by pancreatic enzymes, Eur J Pharm Sci, 41, 376, 10.1016/j.ejps.2010.07.005
Cirri, 2006, Simultaneous effect of cyclodextrin complexation, pH, and hydrophilic polymers on naproxen solubilization, J Pharm Biomed Anal, 42, 126, 10.1016/j.jpba.2005.11.029
Clement, 1992, Tissue distribution and plasma clearance of a novel microcrystalline-coated flurbiprofen formulation, Pharmacologist, 34, 204
Cohen, 1990, Rapid (1 hour) high performance gel filtration chromatography resolves coexisting simple micelles, mixed micelles, and vesicles in bile, J Lipid Res, 31, 2103, 10.1016/S0022-2275(20)42275-8
Cole, 2008, Challenges and opportunities in the encapsulation of liquid and semi-solid formulations into capsules for oral administration, Adv Drug Deliv Rev, 60, 747, 10.1016/j.addr.2007.09.009
Colombo, 1996, Paclitaxel induces significant changes in epidoxorubicin distribution in mice, Ann Oncol, 7, 801, 10.1093/oxfordjournals.annonc.a010758
Constantinides, 2007, Lipid formulation strategies for enhancing intestinal transport and absorption of P-glycoprotein (P-gp) substrate drugs: in vitro/in vivo case studies, J Pharm Sci, 96, 235, 10.1002/jps.20780
Constantinides, 1996, Water-in-oil microemulsions containing medium-chain fatty acids/salts: formulation and intestinal absorption enhancement evaluation, Pharm Res, 13, 210, 10.1023/A:1016030812272
Coon, 1991, Solutol HS 15, nontoxic polyoxyethylene esters of 12-hydroxystearic acid, reverses multidrug resistance, Cancer Res, 51, 897
Corrigan, 1986, Retardation of polymeric carrier dissolution by dispersed drugs: factors influencing the dissolution of solid dispersions containing polyethylene glycols, Drug Dev Ind Pharm, 12, 1777, 10.3109/03639048609042609
Corrigan OI (2007) Salt forms: pharmaceutical aspects, in Encyclopedia of Pharmaceutical Technology ( Swarbrick J ed) pp 3177–3188, Informa Healthcare , New York.
Corrigan, 2002, Comparative physicochemical properties of hydrocortisone-PVP composites prepared using supercritical carbon dioxide by the GAS anti-solvent recrystallization process, by coprecipitation and by spray drying, Int J Pharm, 245, 75, 10.1016/S0378-5173(02)00326-5
Corrigan, 1982, Mechanism of drug dissolution rate enhancement from beta-cyclodextrin-drug systems, J Pharm Pharmacol, 34, 621, 10.1111/j.2042-7158.1982.tb04689.x
Cotton, 1994, L-649,923—the selection of an appropriate salt form and preparation of a stable oral formulation, Int J Pharm, 109, 237, 10.1016/0378-5173(94)90386-7
Cox, 1991, Plasma compatibility of injectables: comparison of intravenous U-74006F, a 21-aminosteroid antioxidant, with dilantin brand of parenteral phenytoin, J Pharm Sci, 80, 371, 10.1002/jps.2600800418
Craig, 1990, Polyethyelene glycols and drug release, Drug Dev Ind Pharm, 16, 2501, 10.3109/03639049009058544
Craig, 1992, Applications of low-frequency dielectric-spectroscopy to the pharmaceutical sciences, Drug Dev Ind Pharm, 18, 1207, 10.3109/03639049209046328
Craig, 2002, The mechanisms of drug release from solid dispersions in water-soluble polymers, Int J Pharm, 231, 131, 10.1016/S0378-5173(01)00891-2
Craig, 1992, The dissolution of nortriptyline HCl from polyethylene-glycol solid dispersions, Int J Pharm, 78, 175, 10.1016/0378-5173(92)90368-C
Crew MD Friesen DT Hancock BC Macri C Nightingale JA Shanker R (2007), inventors
Pfizer, Inc., assignee. Pharmaceutical compositions of a sparingly soluble glycogen phosphorylase inhibitor U.S. patent 7,235,260. 2007 June 26.
Cromwell, 1985, Cyclodextrin adamantanecarboxylate inclusion complexes: studies of the variation in cavity size, J Phys Chem, 89, 326, 10.1021/j100248a029
Crounse, 1961, Human pharmacology of griseofulvin: the effect of fat intake on gastrointestinal absorption, J Invest Dermatol, 37, 529, 10.1038/jid.1961.154
Crowley, 2001, The use of thermal methods for predicting glass-former fragility, Thermochim Acta, 380, 79, 10.1016/S0040-6031(01)00662-1
Cuiné, 2007, Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs, Pharm Res, 24, 748, 10.1007/s11095-006-9194-z
Curatolo, 2009, Utility of hydroxypropylmethylcellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI milieu, Pharm Res, 26, 1419, 10.1007/s11095-009-9852-z
D’Addio, 2011, Controlling drug nanoparticle formation by rapid precipitation, Adv Drug Deliv Rev, 63, 417, 10.1016/j.addr.2011.04.005
Dahan, 2006, Use of a dynamic in vitro lipolysis model to rationalize oral formulation development for poor water soluble drugs: correlation with in vivo data and the relationship to intra-enterocyte processes in rats, Pharm Res, 23, 2165, 10.1007/s11095-006-9054-x
Dahan, 2007, The effect of different lipid based formulations on the oral absorption of lipophilic drugs: the ability of in vitro lipolysis and consecutive ex vivo intestinal permeability data to predict in vivo bioavailability in rats, Eur J Pharm Biopharm, 67, 96, 10.1016/j.ejpb.2007.01.017
Dahan, 2010, The solubility-permeability interplay in using cyclodextrins as pharmaceutical solubilizers: mechanistic modeling and application to progesterone, J Pharm Sci, 99, 2739, 10.1002/jps.22033
Dai, 2010, In vitro methods to assess drug precipitation, Int J Pharm, 393, 1, 10.1016/j.ijpharm.2010.03.040
Dai, 2008, Combination of pluronic/vitamin E TPGS as a potential inhibitor of drug precipitation, Int J Pharm, 355, 31, 10.1016/j.ijpharm.2007.12.015
Dai, 2008, Advanced screening assays to rapidly identify solubility-enhancing formulations: high-throughput, miniaturization and automation, Adv Drug Deliv Rev, 60, 657, 10.1016/j.addr.2007.10.017
Dannenfelser, 1996, Parenteral formulation of flavopiridol (NSC-649890), PDA J Pharm Sci Technol, 50, 356
Danson, 2004, Phase I dose escalation and pharmacokinetic study of pluronic polymer-bound doxorubicin (SP1049C) in patients with advanced cancer, Br J Cancer, 90, 2085, 10.1038/sj.bjc.6601856
Dantuluri, 2011, Role of α-relaxation on crystallization of amorphous celecoxib above Tg probed by dielectric spectroscopy, Mol Pharm, 8, 814, 10.1021/mp100411v
Date, 2008, Parenteral microemulsions: an overview, Int J Pharm, 355, 19, 10.1016/j.ijpharm.2008.01.004
Datta, 2004, Crystal structures of drugs: advances in determination, prediction and engineering, Nat Rev Drug Discov, 3, 42, 10.1038/nrd1280
David, 2012, Impact of the counterion on the solubility and physicochemical properties of salts of carboxylic acid drugs, Drug Dev Ind Pharm, 38, 93, 10.3109/03639045.2011.592530
Davies, 1953, Thermodynamic and kinetic properties of glasses, Adv Phys, 2, 370, 10.1080/00018735300101252
Day, 2010, Label-free imaging of lipophilic bioactive molecules during lipid digestion by multiplex coherent anti-Stokes Raman scattering microspectroscopy, J Am Chem Soc, 132, 8433, 10.1021/ja102069d
de Garavilla L Liversidge EM Liversidge GG (1998), inventors
Nanosystems LLC, assignee. Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions. US Patent 5,835,025. 1998 Nov 10.
de Garavilla, 1996, Controlling the acute hemodynamic effects associated with IV administration of particulate drug dispersions in dogs, Drug Dev Res, 37, 86, 10.1002/(SICI)1098-2299(199602)37:2<86::AID-DDR4>3.0.CO;2-H
D’Errico, 2005, Effect of glycerol on micelle formation by ionic and nonionic surfactants at 25 degrees C, J Colloid Interface Sci, 286, 747, 10.1016/j.jcis.2005.01.030
Desai PR Jain NJ Sharma RK Bahadur P (2001) Effect of additives on the micellization of PEO/PPO/PEO block copolymer F127 in aqueous solution. Colloids and Surfaces Physicochem Eng Aspects 178:57–69.
Descamps, 2007, Transformation of pharmaceutical compounds upon milling and comilling: the role of T(g), J Pharm Sci, 96, 1398, 10.1002/jps.20939
Desiraju, 2010, Crystal engineering: a brief overview, J Chem Sci, 122, 667, 10.1007/s12039-010-0055-2
de Waard, 2011, Bottom-up preparation techniques for nanocrystals of lipophilic drugs, Pharm Res, 28, 1220, 10.1007/s11095-010-0323-3
Di L Fish PV Mano T (2012) Bridging solubility between drug discovery and development. Drug Discov Today 17:486–495.
Dias, 2003, The effect of beta-cyclodextrins on the permeation of diclofenac from supersaturated solutions, Int J Pharm, 263, 173, 10.1016/S0378-5173(03)00366-1
di Cagno, 2011, Solubilization of ibuprofen with β-cyclodextrin derivatives: energetic and structural studies, J Pharm Biomed Anal, 55, 446, 10.1016/j.jpba.2011.02.022
Di Maio, 2011, Gastrointestinal contents in fasted state and post-lipid ingestion: in vivo measurements and in vitro models for studying oral drug delivery, J Control Release, 151, 110, 10.1016/j.jconrel.2010.11.034
DiNunzio, 2010, Applications of KinetiSol dispersing for the production of plasticizer free amorphous solid dispersions, Eur J Pharm Sci, 40, 179, 10.1016/j.ejps.2010.03.002
DiNunzio, 2010, Fusion processing of itraconazole solid dispersions by kinetisol dispersing: a comparative study to hot melt extrusion, J Pharm Sci, 99, 1239, 10.1002/jps.21893
Dixit, 2010, Optimized microemulsions and solid microemulsion systems of simvastatin: characterization and in vivo evaluation, J Pharm Sci, 99, 4892, 10.1002/jps.22208
Do, 2011, The conflict between in vitro release studies in human biorelevant media and the in vivo exposure in rats of the lipophilic compound fenofibrate, Int J Pharm, 414, 118, 10.1016/j.ijpharm.2011.05.009
Dobbins, 1971, Intestinal mucosal lacteal in transport of macromolecules and chylomicrons, Am J Clin Nutr, 24, 77, 10.1093/ajcn/24.1.77
Dobbs, 1987, Modification of supercritical fluid phase-behavior using polar cosolvents, Ind Eng Chem Res, 26, 56, 10.1021/ie00061a011
Doherty, 1987, Mechanisms of dissolution of frusemide/PVP solid dispersions, Int J Pharm, 34, 197, 10.1016/0378-5173(87)90180-3
Dollo, 1999, Improvement in solubility and dissolution rate of 1, 2-dithiole-3-thiones upon complexation with beta-cyclodextrin and its hydroxypropyl and sulfobutyl ether-7 derivatives, J Pharm Sci, 88, 889, 10.1021/js990067o
Dollo, 2003, Spray-dried redispersible oil-in-water emulsion to improve oral bioavailability of poorly soluble drugs, Eur J Pharm Sci, 19, 273, 10.1016/S0928-0987(03)00134-9
Dong, 2008, Solubilization and preformulation of poorly water soluble and hydrolysis susceptible N-epoxymethyl-1,8-naphthalimide (ENA) compound, Int J Pharm, 356, 130, 10.1016/j.ijpharm.2008.01.013
Dontireddy, 2011, A comparative study of spray-dried and freeze-dried hydrocortisone/polyvinyl pyrrolidone solid dispersions, Drug Dev Ind Pharm, 37, 1141, 10.3109/03639045.2011.562213
Dordunoo, 1991, Preformulation studies on solid dispersions containing triamterene or temazepam in polyethylene glycols or Gelucire 44/14 for liquid filling of hard gelatin capsules, Drug Dev Ind Pharm, 17, 1685, 10.3109/03639049109057315
Doshi, 1997, Carbamazepine and polyethylene glycol solid dispersions: preparation, in vitro dissolution, and characterization, Drug Dev Ind Pharm, 23, 1167, 10.3109/03639049709146154
Douglas, 1987, Nanoparticles in drug delivery, Crit Rev Ther Drug Carrier Syst, 3, 233
Dressman, 2007, Estimating drug solubility in the gastrointestinal tract, Adv Drug Deliv Rev, 59, 591, 10.1016/j.addr.2007.05.009
Dubois, 1985, Similarities in the release rates of different drugs from polyethylene glycol 6000 solid dispersions, J Pharm Pharmacol, 37, 494, 10.1111/j.2042-7158.1985.tb03048.x
Ehninger, 1995, Use of a water-soluble busulfan formulation: pharmacokinetic studies in a canine model, Blood, 85, 3247, 10.1182/blood.V85.11.3247.bloodjournal85113247
Elamin, 1994, Increased metastable solubility of milled griseofulvin, depending on the formation of a disordered surface-structure, Int J Pharm, 111, 159, 10.1016/0378-5173(94)00132-4
Eldem, 1991, Optimization of spray-dried and -congealed lipid micropellets and characterization of their surface morphology by scanning electron microscopy, Pharm Res, 8, 47, 10.1023/A:1015874121860
Elder, 2010, The utility of sulfonate salts in drug development, J Pharm Sci, 99, 2948, 10.1002/jps.22058
El-Eini, 1976, Micellar size, shape, and hydration of long-chain polyoxyethylene nonionic surfactants, J Colloid Interface Sci, 54, 348, 10.1016/0021-9797(76)90314-3
Eli, 2000, Determination of association constants of cyclodextrin-nonionic surfactant inclusion complexes by a partition coefficient method, J Incl Phenom Macrocycl Chem, 38, 37, 10.1023/A:1008123930479
El-Sayed, 1983, Solubilization and stabilization of an investigational antineoplastic drug (NSC No 278214) in an intravenous formulation using an emulsion vehicle, Int J Pharm, 13, 303, 10.1016/0378-5173(83)90079-0
Elworthy PH Florence AT Macfarlane CB (1968) Solubilization by Surface Active Agents and Its Applications in Chemistry and Biological Sciences, Chapman and Hall, London.
Elworthy, 1982, Demonstration of maximum solubilization in a polyoxyethylene alkyl ether series of non-ionic surfactants, J Pharm Pharmacol, 34, 543, 10.1111/j.2042-7158.1982.tb04790.x
Elworthy PH Treon JF (1966) Physiological activity of nonionic surfactants, in Nonionic Surfactants ( Schick JM ed) pp 923–970, Marcel Dekker, New York.
European Medicines Agency (EMEA) (2007) CHMP Assessment Report for Viracept, EMEA/CHMP/492059, 20 September 2007. Committee for Medicinal Products for Human Use (CHMP), London.
Endemann, 1993, CD36 is a receptor for oxidized low density lipoprotein, J Biol Chem, 268, 11811, 10.1016/S0021-9258(19)50272-1
Erlich, 1999, Relative bioavailability of danazol in dogs from liquid-filled hard gelatin capsules, Int J Pharm, 179, 49, 10.1016/S0378-5173(98)00386-X
Ernst, 1980, Biological effects of surfactants. IV. Effects of non-ionics and amphoterics on HeLa cells, Toxicology, 15, 233, 10.1016/0300-483X(80)90056-6
Esnaashari, 2005, The use of microviscometry to study polymer dissolution from solid dispersion drug delivery systems, Int J Pharm, 292, 227, 10.1016/j.ijpharm.2004.11.036
Evans, 2000, Naphthalene complexation by beta-cyclodextrin: influence of added short chain branched and linear alcohols, J Incl Phenom Macrocycl Chem, 38, 381, 10.1023/A:1008187916379
Fahelelbom, 1993, Micellar solubilization of clofazimine analogues in aqueous solutions of ionic and nonionic surfactants, Pharm Res, 10, 631, 10.1023/A:1018978809545
Fatouros, 2007, Morphological observations on a lipid-based drug delivery system during in vitro digestion, Eur J Pharm Sci, 31, 85, 10.1016/j.ejps.2007.02.009
Fatouros, 2007, Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro lipid digestion monitored by small-angle X-ray scattering, Pharm Res, 24, 1844, 10.1007/s11095-007-9304-6
Fatouros, 2008, In vitro lipid digestion models in design of drug delivery systems for enhancing oral bioavailability, Expert Opin Drug Metab Toxicol, 4, 65, 10.1517/17425255.4.1.65
Fatouros, 2008, In vitro-in vivo correlations of self-emulsifying drug delivery systems combining the dynamic lipolysis model and neuro-fuzzy networks, Eur J Pharm Biopharm, 69, 887, 10.1016/j.ejpb.2008.01.022
Faucci, 2000, 1H-NMR and molecular modelling techniques for the investigation of the inclusion complex of econazole with alpha-cyclodextrin in the presence of malic acid, J Pharm Biomed Anal, 23, 25, 10.1016/S0731-7085(00)00260-0
Ferguson, 1976, The effect of surfactants upon mammalian cells in vitro, Food Cosmet Toxicol, 14, 431, 10.1016/S0015-6264(76)80181-2
Fernandes, 2002, Physicochemical characterization and in vitro dissolution behavior of nicardipine-cyclodextrins inclusion compounds, Eur J Pharm Sci, 15, 79, 10.1016/S0928-0987(01)00208-1
Fernandez, 2009, In vitro gastrointestinal lipolysis of four formulations of piroxicam and cinnarizine with the self emulsifying excipients Labrasol and Gelucire 44/14, Pharm Res, 26, 1901, 10.1007/s11095-009-9906-2
Fernandez, 2007, Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol (R), medium chain glycerides and PEG esters, Biochimica et Biophysica Acta—Mol Cell Biol Lipids, 1771, 633, 10.1016/j.bbalip.2007.02.009
Fernandez S Rodier JD Ritter N Mahler B Demarne F Carrière F Jannin V (2008) Lipolysis of the semi-solid self-emulsifying excipient Gelucire 44/14 by digestive lipases. Biochim Biophys Acta (Amsterdam) 1781:367–375.
Fini, 1999, Formation of ion-pairs in aqueous solutions of diclofenac salts, Int J Pharm, 187, 163, 10.1016/S0378-5173(99)00180-5
Fini, 1996, Factors governing the dissolution of diclofenac salts, Eur J Pharm Sci, 4, 231, 10.1016/0928-0987(95)00051-8
Fini, 2002, Ultrasound-compacted and spray-congealed indomethacin/polyethyleneglycol systems, Int J Pharm, 247, 11, 10.1016/S0378-5173(02)00327-7
Fleischman, 2003, Crystal engineering of the composition of pharmaceutical phases: multiple-component crystalline solids involving carbamazepine, Cryst Growth Des, 3, 909, 10.1021/cg034035x
Flory PJ (1953) Principles of Polymer Chemistry, Cornell University Press, Ithaca, NY.
Flourié, 1993, Fate of beta-cyclodextrin in the human intestine, J Nutr, 123, 676, 10.1093/jn/123.4.676
Floyd, 1999, Top ten considerations in the development of parenteral emulsions, Pharm Sci Technol Today, 4, 134, 10.1016/S1461-5347(99)00141-8
Flynn, 1980, Buffers: pH control within pharmaceutical systems, J Parenter Drug Assoc, 34, 139
Flynn, 1979, Cholesterol solubility in organic solvents, J Pharm Sci, 68, 1090, 10.1002/jps.2600680908
Forbes, 1995, Dissolution kinetics and solubilities of p-aminosalicylic acid and its salts, Int J Pharm, 126, 199, 10.1016/0378-5173(95)04126-5
Ford, 1979, Ageing of indomethacin-polyethylene glycol 6000 solid dispersion, Pharm Acta Helv, 54, 353
Forester, 1983, Rat intestine secretes spherical high density lipoproteins, J Biol Chem, 258, 5938, 10.1016/S0021-9258(20)81987-5
Forster, 2001, The potential of small-scale fusion experiments and the Gordon-Taylor equation to predict the suitability of drug/polymer blends for melt extrusion, Drug Dev Ind Pharm, 27, 549, 10.1081/DDC-100105180
Forster, 2001, Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis, Int J Pharm, 226, 147, 10.1016/S0378-5173(01)00801-8
Fort, 1984, Hemolysis study of aqueous polyethylene glycol 400, propylene glycol and ethanol combinations in vivo and in vitro, J Parenter Sci Technol, 38, 82
Frank, 1976, Cyclodextrin nephrosis in the rat, Am J Pathol, 83, 367
Freundlich H (1909) Kapillarchemie. p 144, Akademische Yerlagsgesellschaft, Leipzig, Germany.
Friche, 1990, The solvents cremophor EL and Tween 80 modulate daunorubicin resistance in the multidrug resistant Ehrlich ascites tumor, Cancer Commun, 2, 297
Friche, 1990, The solvents cremophor EL and Tween 80 modulate daunorubicin resistance in the multidrug resistant Ehrlich ascites tumor, Cancer Commun, 2, 297
Friesen, 2008, Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: an overview, Mol Pharm, 5, 1003, 10.1021/mp8000793
Friščić, 2010, Benefits of cocrystallisation in pharmaceutical materials science: an update, J Pharm Pharmacol, 62, 1547, 10.1111/j.2042-7158.2010.01133.x
Fu, 1987, The biocompatibility of parenteral vehicles: in vitro/in vivo screening comparison and the effect of excipients on hemolysis, J Parenter Sci Technol, 41, 164
Fukuda, 2008, Influence of sulfobutyl ether beta-cyclodextrin (Captisol) on the dissolution properties of a poorly soluble drug from extrudates prepared by hot-melt extrusion, Int J Pharm, 350, 188, 10.1016/j.ijpharm.2007.08.038
Fusaro, 2005, Dense gas antisolvent precipitation: a comparative investigation of the GAS and PCA techniques, Ind Eng Chem Res, 44, 1502, 10.1021/ie049495h
Galcera, 2009, Effect of the counterion on the solubility of isostructural pharmaceutical lamotrigine salts, Cryst Growth Des, 9, 327, 10.1021/cg8005025
Gallo-Torres, 1978, The effect of medium-chain triglycerides on the bioavailability of vitamin E, Int J Vitam Nutr Res, 48, 240
Ganta, 2009, Formulation and pharmacokinetic evaluation of an asulacrine nanocrystalline suspension for intravenous delivery, Int J Pharm, 367, 179, 10.1016/j.ijpharm.2008.09.022
Gao, 2011, Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: Performance and mechanism, J Control Release, 149, 168, 10.1016/j.jconrel.2010.10.013
Gao, 2011, Preparation of a chemically stable quercetin formulation using nanosuspension technology, Int J Pharm, 404, 231, 10.1016/j.ijpharm.2010.11.009
Gao, 2008, Amorphous pharmaceutical solids: characterization, stabilization, and development of marketable formulations of poorly soluble drugs with improved oral absorption, Mol Pharm, 5, 903, 10.1021/mp800203k
Gao, 2009, Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption, J Pharm Sci, 98, 516, 10.1002/jps.21451
Gao, 2006, Development of supersaturatable self-emulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs, Expert Opin Drug Deliv, 3, 97, 10.1517/17425247.3.1.97
Gao, 2011, Preparation and characterization of intravenously injectable curcumin nanosuspension, Drug Deliv, 18, 131, 10.3109/10717544.2010.520353
Gao, 2010, Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer, Drug Dev Ind Pharm, 36, 1225, 10.3109/03639041003695139
Gao, 2010, Physicochemical and pharmacokinetic characterization of a spray-dried cefpodoxime proxetil nanosuspension, Chem Pharm Bull (Tokyo), 58, 912, 10.1248/cpb.58.912
Garren, 1990, Aqueous solubility properties of a dibasic peptide-like compound, Int J Pharm, 63, 167, 10.1016/0378-5173(90)90167-3
Gassmann, 1994, Hydrosols: alternatives for the parenteral application of poorly water-soluble drugs, Eur J Pharm Biopharm, 40, 64
Gershkovich, 2009, The role of molecular physicochemical properties and apolipoproteins in association of drugs with triglyceride-rich lipoproteins: in-silico prediction of uptake by chylomicrons, J Pharm Pharmacol, 61, 31, 10.1211/jpp.61.01.0005
Ghosh, 2011, Comparison of HPMC based polymers performance as carriers for manufacture of solid dispersions using the melt extruder, Int J Pharm, 419, 12, 10.1016/j.ijpharm.2011.05.073
Gibaud, 2005, Melarsoprol-cyclodextrins inclusion complexes, Int J Pharm, 306, 107, 10.1016/j.ijpharm.2005.09.003
Gibson L (2007) Lipid-based excipients for oral drug delivery, in Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water Soluble Drugs ( Hauss DJ ed) pp 1–31, Informa Healthcare, Inc., New York.
Gilis PA de Conde V Vandecruys R (1997), inventors
Janssen Pharmaceutica NV, assignee. Beads Having a Core Coated with an Antifungal and a Polymer, U.S. patent 5633015. 1997 May 27.
Giron D Grant DJW (2002) Evaluation of solid-state properties of salts, in Handbook of Pharmaceutical Salts: Properties, Selection and Use ( Stahl PH Wermuth GH eds) pp 40–81, Wiley-VCH, Weinheim, Germany.
Good, 2011, Dependence of cocrystal formation and thermodynamic stability on moisture sorption by amorphous polymer, CrystEngComm, 13, 1181, 10.1039/C0CE00592D
Good, 2009, Solubility advantage of pharmaceutical cocrystals, Cryst Growth Des, 9, 2252, 10.1021/cg801039j
Goole, 2010, The effects of excipients on transporter mediated absorption, Int J Pharm, 393, 17, 10.1016/j.ijpharm.2010.04.019
Gordon, 1952, Ideal copolymers and the 2nd-order transitions of synthetic rubbers. 1. Non-crystalline copolymers, Journal of Applied Chemistry, 2, 493, 10.1002/jctb.5010020901
Gordon, 1987, Effect of tablet solubility and hygroscopicity on disintegrant efficiency in direct compression tablets in terms of dissolution, J Pharm Sci, 76, 907, 10.1002/jps.2600761213
Gordon, 1990, The effect of aging on disintegrant efficiency in direct compression tablets with varied solubility and hygroscopicity, in terms of dissolution, Drug Dev Ind Pharm, 16, 437, 10.3109/03639049009114896
Graeser, 2009, Correlating thermodynamic and kinetic parameters with amorphous stability, Eur J Pharm Sci, 37, 492, 10.1016/j.ejps.2009.04.005
Grant DJW Higuchi T (1990) Solubility Behavior of Organic Compounds, Wiley-Interscience, New York.
Grantscharova, 1986, Vapor-pressure, solubility and affinity of undercooled melts and glasses, J Non-Cryst Solids, 81, 99, 10.1016/0022-3093(86)90261-9
Greenhalgh, 1999, Solubility parameters as predictors of miscibility in solid dispersions, J Pharm Sci, 88, 1182, 10.1021/js9900856
Griffin, 1949, Classification of surface-active agents by HLB, J Soc Cosmet Chem, 1, 311
Gross, 2007, An approach to early-phase salt selection: application to NBI-75043, Org Process Res Dev, 11, 365, 10.1021/op060221a
Grove, 2006, Bioavailability of seocalcitol II: development and characterisation of self-microemulsifying drug delivery systems (SMEDDS) for oral administration containing medium and long chain triglycerides, Eur J Pharmaceutical Sci, 28, 233, 10.1016/j.ejps.2006.02.005
Grove, 2005, Bioavailability of seocalcitol I. Relating solubility in biorelevant media with oral bioavailability in rats: effect of medium and long chain triglycerides, J Pharm Sci, 94, 1830, 10.1002/jps.20403
Groves, 1976, The self-emulsifying action of mixed surfactants in oil, Acta Pharm Suec, 13, 361
Grunenberg, 1996, Theoretical derivation and practical application of energy temperature diagrams as an instrument in preformulation studies of polymorphic drug substances, Int J Pharm, 129, 147, 10.1016/0378-5173(95)04283-0
Grzybowska, 2010, Molecular dynamics and physical stability of amorphous anti-inflammatory drug: celecoxib, J Phys Chem B, 114, 12792, 10.1021/jp1040212
Gu, 2005, Using a novel multicompartment dissolution system to predict the effect of gastric pH on the oral absorption of weak bases with poor intrinsic solubility, J Pharm Sci, 94, 199, 10.1002/jps.20242
Guerrieri, 2010, Analysis of relationships between solid-state properties, counterion, and developability of pharmaceutical salts, AAPS PharmSciTech, 11, 1212, 10.1208/s12249-010-9499-4
Guerrieri, 2009, Role of salt and excipient properties on disproportionation in the solid-state, Pharm Res, 26, 2015, 10.1007/s11095-009-9918-y
Gupta, 2001, Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent, Pharm Dev Technol, 6, 563, 10.1081/PDT-120000294
Gupta, 2002, Hydrogen bonding with adsorbent during storage governs drug dissolution from solid-dispersion granules, Pharm Res, 19, 1663, 10.1023/A:1020905412654
Gupta, 2003, Formation of physically stable amorphous drugs by milling with Neusilin, J Pharm Sci, 92, 536, 10.1002/jps.10308
Gupta, 2004, Stability and solubility of celecoxib-PVP amorphous dispersions: a molecular perspective, Pharm Res, 21, 1762, 10.1023/B:PHAM.0000045226.42859.b8
Gupta, 1996, Non-crystalline solids: glasses and amorphous solids, J Non-Cryst Solids, 195, 158, 10.1016/0022-3093(95)00502-1
Gupta, 1990, Effect of food on the pharmacokinetics of cyclosporine in healthy subjects following oral and intravenous administration, J Clin Pharmacol, 30, 643, 10.1002/j.1552-4604.1990.tb01868.x
Gupta, 1990, High-fat meals increase the clearance of cyclosporine, Pharm Res, 7, 46, 10.1023/A:1015831408425
Guyot, 1995, Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion-compounds and peg solid dispersions, Int J Pharm, 123, 53, 10.1016/0378-5173(95)00039-L
Guzmán H Tawa M Zhang Z Ratanabanangkoon P Shaw P Mustonen P Gardner CR Chen H Moreau JP Almarsson O (2004) A “spring and parachute” approach to designing solid celecoxib formulations having enhanced oral absorption (Abstract). AAPS PharmSciTech T2189.
Guzmán, 2007, Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of celecoxib from solid oral formulations, J Pharm Sci, 96, 2686, 10.1002/jps.20906
Gwak, 2005, Enhanced bioavailability of piroxicam via salt formation with ethanolamines, Int J Pharm, 297, 156
Hajratwala, 1982, Particle size reduction by a hammer mill. I. Effect of output screen size, feed particle size, and mill speed, J Pharm Sci, 71, 188, 10.1002/jps.2600710212
Hall DG Pethica BA (1967) Thermodynamics of micelle formation, in Nonionic Surfactants ( Schick JM ed) pp 516–557, Marcel Dekker, New York.
Hamosh, 1973, Lingual lipase and its role in the digestion of dietary lipid, J Clin Invest, 52, 88, 10.1172/JCI107177
Han, 2011, Enhanced dissolution and bioavailability of biochanin A via the preparation of solid dispersion: in vitro and in vivo evaluation, Int J Pharm, 415, 89, 10.1016/j.ijpharm.2011.05.055
Han, 2009, Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: effects of lipid composition and formulation, Int J Pharm, 379, 18, 10.1016/j.ijpharm.2009.06.001
Hanna M York P (1998), inventors
University of Bradford, West Yorkshire, UK, assignee. Method and apparatus for the formulation of particles. US Patent 5851453. 1998 Dec 22.
Hansen, 2004, Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid, Int J Pharm, 287, 55, 10.1016/j.ijpharm.2004.08.014
Hardung, 2010, Combining HME & solubilization: Soluplus—the solid solution, Drug Delivery Technol, 10, 20
Hargrove, 1989, Absorption of oral progesterone is influenced by vehicle and particle size, Am J Obstet Gynecol, 161, 948, 10.1016/0002-9378(89)90759-X
Harrison, 1982, Cyclodextrin adamantanecarboxylate inclusion complexes: a model system for the hydrophobic effect, Biopolymers, 21, 1153, 10.1002/bip.360210611
Hasa, 2011, Enhanced oral bioavailability of vinpocetine through mechanochemical salt formation: physico-chemical characterization and in vivo studies, Pharm Res, 28, 1870, 10.1007/s11095-011-0415-8
Hasegawa, 1985, Bioavailability and stability of nifedipine-enteric coating agent solid dispersion, Chem Pharm Bull (Tokyo), 33, 388, 10.1248/cpb.33.388
Hastewell, 1994, Enhancement of human calcitonin absorption across the rat colon in vivo, Int J Pharm, 101, 115, 10.1016/0378-5173(94)90082-5
Haynes, 2004, Supramolecular synthon competition in organic sulfonates: a CSD survey, Cryst Eng Comm, 6, 584, 10.1039/b413797c
He, 2003, Solubilization of fluasterone in cosolvent/cyclodextrin combinations, Int J Pharm, 264, 25, 10.1016/S0378-5173(03)00389-2
He, 2006, Solubilization of two structurally related anticancer drugs: XK-469 and PPA, J Pharm Sci, 95, 97, 10.1002/jps.20500
Hecq, 2005, Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine, Int J Pharm, 299, 167, 10.1016/j.ijpharm.2005.05.014
Hecq, 2006, Preparation and in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3, a highly dosed poorly water-soluble weak base, Eur J Pharm Biopharm, 64, 360, 10.1016/j.ejpb.2006.05.008
Henck, 2007, Designing a molecular delivery system within a preclinical timeframe, Drug Discov Today, 12, 189, 10.1016/j.drudis.2007.01.006
Higuchi T Connons KA (1964) Advances in analytical chemistry and instrumentation, in Advances in Analytical Chemistry and Instrumentation ( Reilly CN ed) pp 117–212, Wiley-Interscience, New York.
Hilkens, 1997, Peripheral neuropathy induced by combination chemotherapy of docetaxel and cisplatin, Br J Cancer, 75, 417, 10.1038/bjc.1997.68
Hirasawa, 1999, Lactose as a low molecular weight carrier of solid dispersions for carbamazepine and ethenzamide, Chem Pharm Bull (Tokyo), 47, 417, 10.1248/cpb.47.417
Hirayama, 1997, Crystallization and polymorphic transition behavior of chloramphenicol palmitate in 2-hydroxypropyl-beta-cyclodextrin matrix, Eur J Pharm Sci, 5, 23, 10.1016/S0928-0987(96)00250-3
Hirayama F Zaoh K Harata K Saenger W Uekama K (2001) Transparent, adhesive film formation of per-O-valeryl-beta-cyclodextrin. Chem Lett 636–637.
Hirsch, 1978, Fenoprofen: drug form selection and preformulation stability studies, J Pharm Sci, 67, 231, 10.1002/jps.2600670227
Hirunpanich, 2008, Inhibitory effect of docosahexaenoic acid (DHA) on the intestinal metabolism of midazolam: in vitro and in vivo studies in rats, Int J Pharm, 351, 133
Hirunpanich, 2006, Docosahexaenoic acid (DHA) inhibits saquinavir metabolism in-vitro and enhances its bioavailability in rats, J Pharm Pharmacol, 58, 651, 10.1211/jpp.58.5.0010
Hirunpanich, 2007, Inhibitory effects of saturated and polyunsaturated fatty acids on the cytochrome P450 3A activity in rat liver microsomes, Biol Pharm Bull, 30, 1586, 10.1248/bpb.30.1586
Hitzenberger, 1974, Comparative studies on the absorption of ampicillin trihydrate and potassium ampicillin, Int J Clin Pharmacol, 9, 114
Ho, 1996, The preparation and characterization of solid dispersions on pellets using a fluidized-bed system, Int J Pharm, 139, 223, 10.1016/0378-5173(96)04594-2
Holm, 2004, Successful in silico predicting of intestinal lymphatic transfer, Int J Pharm, 272, 189, 10.1016/j.ijpharm.2003.12.017
Holm, 2011, Thermodynamics of complexation of tauro- and glyco-conjugated bile salts with two modified beta-cyclodextrins, J Incl Phenom Macrocycl Chem, 69, 201, 10.1007/s10847-010-9831-3
Hong, 2011, Effect of cyclodextrin derivation and amorphous state of complex on accelerated degradation of ziprasidone, J Pharm Sci, 100, 2703, 10.1002/jps.22498
Hsieh, 2012, pH-induced precipitation behavior of weakly basic compounds: determination of extent and duration of supersaturation using potentiometric titration and correlation to solid state properties, Pharm Res, 29, 2738, 10.1007/s11095-012-0759-8
Hu, 2004, Rapid dissolving high potency danazol powders produced by spray freezing into liquid process, Int J Pharm, 271, 145, 10.1016/j.ijpharm.2003.11.003
Hu, 2004, Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs, J Pharm Pharmacol, 56, 1527, 10.1211/0022357044959
Huang, 2011, Interplay of formulation and process methodology on the extent of nifedipine molecular dispersion in polymers, Int J Pharm, 420, 59, 10.1016/j.ijpharm.2011.08.021
Huang, 2010, Effect of micellar solubilization on cocrystal solubility and stability, Cryst Growth Des, 10, 2050, 10.1021/cg1002176
Hughey, 2010, Dissolution enhancement of a drug exhibiting thermal and acidic decomposition characteristics by fusion processing: a comparative study of hot melt extrusion and KinetiSol dispersing, AAPS PharmSciTech, 11, 760, 10.1208/s12249-010-9431-y
Hurter, 1993, Molecular modeling of micelle formation and solubilization in block-copolymer micelles. 1. A self-consistent mean-field lattice theory, Macromolecules, 26, 5592, 10.1021/ma00073a010
Iacocca, 2010, Particle engineering: a strategy for establishing drug substance physical property specifications during small molecule development, J Pharm Sci, 99, 51, 10.1002/jps.21801
Iervolino, 2000, Membrane penetration enhancement of ibuprofen using supersaturation, Int J Pharm, 198, 229, 10.1016/S0378-5173(00)00346-X
Ignatious F Baldoni J (2001), inventors; Smithkline Beecham Corporation, assignee. Electrospun pharmaceutical compositions. Patent WO0154667.
Ignatious F Sun L (2004), inventors; Smithkline Beecham Corporation, assignee. Electrospun amorphous pharmaceutical compositions, Patent WO 2004014304.
Ignatious, 2010, Electrospun nanofibers in oral drug delivery, Pharm Res, 27, 576, 10.1007/s11095-010-0061-6
Ikeda, 1977, Micellar interaction of tetracycline antibiotics, Chem Pharm Bull (Tokyo), 25, 1067, 10.1248/cpb.25.1067
Inoue, 1993, Thermodynamics of molecular recognition by cyclodextrins. 2. Calorimetric titration of inclusion complexation with modified beta-cyclodextrins: enthalpy-entropy compensation in host-guest complexation: from ionophore to cyclodextrin and cyclophane, J Am Chem Soc, 115, 10637, 10.1021/ja00076a023
Ishikawa, 2011, Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry, J Med Chem, 54, 1539, 10.1021/jm101356p
Ishikawa, 2005, Interaction of modified cyclodextrins with cytochrome P-450, Biosci Biotechnol Biochem, 69, 246, 10.1271/bbb.69.246
Islam, 1993, Solubility, stability and ionization behaviour of famotidine, J Pharm Pharmacol, 45, 682, 10.1111/j.2042-7158.1993.tb07088.x
Ismail, 1970, Micellar solubilization of barbiturates. I. Solubilities of certain barbiturates in polysorbates of varying hydrophobic chain length, J Pharm Sci, 59, 220, 10.1002/jps.2600590216
Ito, 2005, Oral solid gentamicin preparation using emulsifier and adsorbent, J Control Release, 105, 23, 10.1016/j.jconrel.2005.03.017
Ivanova R Alexandridis P Lindman B (2001) Interaction of poloxamer block copolymers with cosolvents and surfactants. Colloids and Surfaces a-Physicochem Eng Aspects 183:41–53.
Jain, 2004, Effect of pH-sodium lauryl sulfate combination on solubilization of PG-300995 (an anti-HIV agent): a technical note, AAPS PharmSciTech, 5, e45, 10.1208/pt050345
Jain, 2010, Importance of early characterization of physicochemical properties in developing high-dose intravenous infusion regimens for poorly water-soluble compounds, PDA J Pharm Sci Technol, 64, 517
Jain NJ Aswal VK Goyal PS Bahadur P (2000) Salt induced micellization and micelle structures of PEO/PPO/PEO block copolymers in aqueous solution. Colloids and Surfaces. a. Physicochemical and Engineering Aspects 173:85–94.
Jain NJ George A Bahadur P (1999) Effect of salt on the micellization of pluronic P65 in aqueous solution. Colloids and Surfaces. A. Physicochemical and Engineering Aspects 157:275–283.
Jambhekar, 2004, The physicochemical characteristics and bioavailability of indomethacin from beta-cyclodextrin, hydroxyethyl-beta-cyclodextrin, and hydroxypropyl-beta-cyclodextrin complexes, Int J Pharm, 270, 149, 10.1016/j.ijpharm.2003.10.012
James, 1985, Kinetics of crystal nucleation in silicate-glasses, J Non-Cryst Solids, 73, 517, 10.1016/0022-3093(85)90372-2
Jannin, 2008, Approaches for the development of solid and semi-solid lipid-based formulations, Adv Drug Deliv Rev, 60, 734, 10.1016/j.addr.2007.09.006
Janssens, 2010, Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and Eudragit e100, Pharm Res, 27, 775, 10.1007/s11095-010-0069-y
Janssens, 2008, Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study, Eur J Pharm Biopharm, 69, 158, 10.1016/j.ejpb.2007.11.004
Janssens, 2009, Review: physical chemistry of solid dispersions, J Pharm Pharmacol, 61, 1571, 10.1211/jpp.61.12.0001
Jantratid, 2009, Biorelevant dissolution media simulating the proximal human gastrointestinal tract: an update, Dissolution Technologies, 16, 21, 10.14227/DT160309P21
Jantratid, 2008, Designing biorelevant dissolution tests for lipid formulations: case example—lipid suspension of RZ-50, Eur J Pharm Biopharm, 69, 776, 10.1016/j.ejpb.2007.12.010
Jarho, 1998, Hydroxypropyl-beta-cyclodextrin and its combination with hydroxypropyl-methylcellulose increases aqueous solubility of delta9-tetrahydrocannabinol, Life Sci, 63, PL381, 10.1016/S0024-3205(98)00528-1
Jenning, 2001, Encapsulation of retinoids in solid lipid nanoparticles (SLN), J Microencapsul, 18, 149, 10.1080/02652040010000361
Jia, 2011, A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate, Eur J Pharm Biopharm, 79, 126, 10.1016/j.ejpb.2011.05.009
Jinno, 2008, In vitro-in vivo correlation for wet-milled tablet of poorly water-soluble cilostazol, J Control Release, 130, 29, 10.1016/j.jconrel.2008.05.013
Johari, 2000, A resolution for the enigma of a liquid’s configurational entropy-molecular kinetics relation, J Chem Phys, 112, 8958, 10.1063/1.481509
Johari, 2011, Mechanical relaxation and the notion of time-dependent extent of ergodicity during the glass transition, Phys Rev E Stat Nonlin Soft Matter Phys, 84, 021501, 10.1103/PhysRevE.84.021501
Johari, 2011, Clausius limits on cooling and heating through the liquid-glass range of three pharmaceuticals and one metal alloy: annealing effects and residual entropy, Thermochim Acta, 522, 173, 10.1016/j.tca.2011.02.017
Johari, 2005, Dielectric studies of molecular motions in amorphous solid and ultraviscous acetaminophen, J Pharm Sci, 94, 2207, 10.1002/jps.20455
Johari, 2010, On determining the relaxation time of glass and amorphous pharmaceuticals' stability from thermodynamic data, Thermochim Acta, 511, 89, 10.1016/j.tca.2010.07.029
Johnson, 2002, An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine, AAPS PharmSci, 4, E40, 10.1208/ps040440
Johnson, 2003, Prediction of precipitation-induced phlebitis: a statistical validation of an in vitro model, J Pharm Sci, 92, 1574, 10.1002/jps.10396
Johnston, 1965, Triglyceride biosynthesis in the intestinal mucosa, Biochim Biophys Acta, 106, 1, 10.1016/0005-2760(65)90089-5
Jones, 1987, The acetotoluides as models for studying cyclodextrin inclusion complexes, Int J Pharm, 36, 223, 10.1016/0378-5173(87)90159-1
Joshi, 2004, Bioavailability enhancement of a poorly water-soluble drug by solid dispersion in polyethylene glycol-polysorbate 80 mixture, Int J Pharm, 269, 251, 10.1016/j.ijpharm.2003.09.002
Jouyban A , (2008). Review of the cosolvency models for predicting solubility of drugs in water-cosolvent mixtures. Journal of Pharmacy and Pharmaceutical Sciences. 11:32–57.
Juhnke, 2010, Accelerated formulation development for nanomilled active pharmaceutical ingredients using a screening approach, Chem Eng Technol, 33, 1412, 10.1002/ceat.201000062
Jun, 2005, Cefuroxime axetil solid dispersions prepared using solution enhanced dispersion by supercritical fluids, J Pharm Pharmacol, 57, 1529, 10.1211/jpp.57.12.0003
Junco, 2002, Optimisation of supercritical carbon dioxide systems for complexation of naproxen: beta-cyclodextrin, J Incl Phenom Macrocycl Chem, 44, 69, 10.1023/A:1023028815180
Jung, 2001, Particle design using supercritical fluids: literature and patent survey, J Supercrit Fluids, 20, 179, 10.1016/S0896-8446(01)00064-X
Jung, 1999, Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique, Int J Pharm, 187, 209, 10.1016/S0378-5173(99)00191-X
Jung, 2010, Bioavailability of indomethacin-saccharin cocrystals, J Pharm Pharmacol, 62, 1560, 10.1111/j.2042-7158.2010.01189.x
Junquera, 1993, Effect of the presence of beta-cyclodextrin on the micellization process of sodium dodecyl-sulfate or sodium perfluorooctanoate in water, Langmuir, 9, 1213, 10.1021/la00029a011
Kadam, 2009, Solubilization of poorly water-soluble drug carbamezapine in pluronic micelles: effect of molecular characteristics, temperature and added salt on the solubilizing capacity, Colloids Surf B Biointerfaces, 72, 141, 10.1016/j.colsurfb.2009.03.027
Kadam, 2011, Micelles from PEO-PPO-PEO block copolymers as nanocontainers for solubilization of a poorly water soluble drug hydrochlorothiazide, Colloids Surf B Biointerfaces, 83, 49, 10.1016/j.colsurfb.2010.10.041
Kaminski, 2011, Do intermolecular interactions control crystallization abilities of glass-forming liquids?, J Phys Chem B, 115, 11537, 10.1021/jp202368b
Kanaujia, 2011, Nanoparticle formation and growth during in vitro dissolution of ketoconazole solid dispersion, J Pharm Sci, 100, 2876, 10.1002/jps.22491
Kapsi, 2001, Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability, Int J Pharm, 229, 193, 10.1016/S0378-5173(01)00867-5
Karavas E Georgarakis E Bikiaris D Thomas T Katsos V Xenakis A (2001) Hydrophilic matrices as carriers in felodipine solid dispersion systems, in Trends in Colloid and Interface Science XV ( Koutsoukos PG ed) pp 149–152, Springer, Berlin.
Karavas, 2007, Investigation of the release mechanism of a sparingly water-soluble drug from solid dispersions in hydrophilic carriers based on physical state of drug, particle size distribution and drug-polymer interactions, Eur J Pharm Biopharm, 66, 334, 10.1016/j.ejpb.2006.11.020
Karavas, 2005, Miscibility behavior and formation mechanism of stabilized felodipine-polyvinylpyrrolidone amorphous solid dispersions, Drug Dev Ind Pharm, 31, 473, 10.1080/03639040500215958
Karpf, 2006, Effect of different surfactants in biorelevant medium on the secretion of a lipophilic compound in lipoproteins using Caco-2 cell culture, J Pharm Sci, 95, 45, 10.1002/jps.20431
Katneni, 2007, Impact of cremophor-EL and polysorbate-80 on digoxin permeability across rat jejunum: delineation of thermodynamic and transporter related events using the reciprocal permeability approach, J Pharm Sci, 96, 280, 10.1002/jps.20779
Kato, 1981, Relationship between polymorphism and bioavailability of amorbarbital in the rabbit, Chem Pharm Bull (Tokyo), 29, 268, 10.1248/cpb.29.268
Kaukonen, 2004, Drug solubilization behavior during in vitro digestion of suspension formulations of poorly water-soluble drugs in triglyceride lipids, Pharm Res, 21, 254, 10.1023/B:PHAM.0000016283.87709.a9
Kaushal, 2008, Thermodynamic behavior of glassy state of structurally related compounds, Eur J Pharm Biopharm, 69, 1067, 10.1016/j.ejpb.2008.02.001
Kawakami, 2009, Current status of amorphous formulation and other special dosage forms as formulations for early clinical phases, J Pharm Sci, 98, 2875, 10.1002/jps.21816
Kearney, 1992, The effect of cyclodextrins on the rate of intramolecular lactamization of gabapentin in aqueous-solution, Int J Pharm, 78, 25, 10.1016/0378-5173(92)90351-2
Kemper, 2003, Increased penetration of paclitaxel into the brain by inhibition of P-glycoprotein, Clin Cancer Res, 9, 2849
Kennedy, 2008, Enhanced bioavailability of a poorly soluble VR1 antagonist using an amorphous solid dispersion approach: a case study, Mol Pharm, 5, 981, 10.1021/mp800061r
Kerc, 1995, Thermal-analysis of glassy pharmaceuticals, Thermochim Acta, 248, 81, 10.1016/0040-6031(94)01949-H
Kerc, 1998, Alternative solvent-free preparation methods for felodipine surface solid dispersions, Drug Dev Ind Pharm, 24, 359, 10.3109/03639049809085631
Kesisoglou, 2008, Understanding the effect of API properties on bioavailability through absorption modeling, AAPS J, 10, 516, 10.1208/s12248-008-9061-4
Khalafallah, 1974, Bioavailability determination of two crystal forms of sulfameter in humans from urinary excretion data, J Pharm Sci, 63, 861, 10.1002/jps.2600630611
Khan, 2011, Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000, J Pharm Sci, 100, 4281, 10.1002/jps.22613
Khoo, 2000, The formulation of halofantrine as either non-solubilizing PEG 6000 or solubilizing lipid based solid dispersions: physical stability and absolute bioavailability assessment, Int J Pharm, 205, 65, 10.1016/S0378-5173(00)00485-3
Khougaz, 2000, Crystallization inhibition in solid dispersions of MK-0591 and poly(vinylpyrrolidone) polymers, J Pharm Sci, 89, 1325, 10.1002/1520-6017(200010)89:10<1325::AID-JPS10>3.0.CO;2-5
Ki, 2008, The efficacy and safety of clopidogrel resinate as a novel polymeric salt form of clopidogrel, Arch Pharm Res, 31, 250, 10.1007/s12272-001-1149-7
Kim, 2004, Development of parenteral formulation for a novel angiogenesis inhibitor, CKD-732 through complexation with hydroxypropyl-beta-cyclodextrin, Int J Pharm, 272, 79, 10.1016/j.ijpharm.2003.11.034
Kimura, 1975, Thermodynamics of aqueous-solutions of nonelectrolytes. 2. Enthalpies of transfer of 1-methyl-2-pyrrolidinone from water to many aqueous alcohols, J Solution Chem, 4, 241, 10.1007/BF00646561
Kimura, 1999, Solid-state 13C nuclear magnetic resonance spectroscopic study on amorphous solid complexes of tolbutamide with 2-hydroxypropyl-alpha- and -beta-cyclodextrins, Pharm Res, 16, 1729, 10.1023/A:1018958116349
Kindel, 2010, The mechanism of the formation and secretion of chylomicrons, Atheroscler Suppl, 11, 11, 10.1016/j.atherosclerosissup.2010.03.003
Kipp, 2004, The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs, Int J Pharm, 284, 109, 10.1016/j.ijpharm.2004.07.019
Kipp JE (2007) Solubilizing systems for parenteral formulation development - small molecules, in Solvent Systems and Their Selection in Pharmaceutics and Biopharmaceutics ( Augustijns P Brewster M eds) pp 309–336, Springer, New York.
Kipp JE Wong JCTW Doty MJ Rebbeck CL . (2002), inventors
Baxter International Inc., assignee. Microprecipitation method for preparing submicron suspensions U.S. patent 6607784. 2003 Aug 19.
Koester, 2004, Bioavailability of carbamazepine:beta-cyclodextrin complex in beagle dogs from hydroxypropylmethylcellulose matrix tablets, Eur J Pharm Sci, 22, 201, 10.1016/j.ejps.2004.03.010
Koester, 2003, Influence of beta-cyclodextrin complexation on carbamazepine release from hydroxypropyl methylcellulose matrix tablets, Eur J Pharm Biopharm, 55, 85, 10.1016/S0939-6411(02)00127-3
Kojima, 2010, High-throughput cocrystal slurry screening by use of in situ Raman microscopy and multi-well plate, Int J Pharm, 399, 52, 10.1016/j.ijpharm.2010.07.055
Koltun, 2010, Preclinical comparison of intravenous melphalan pharmacokinetics administered in formulations containing either (SBE)7cm-β-cyclodextrin or a co-solvent system, Biopharm Drug Dispos, 31, 450, 10.1002/bdd.725
Komiyama, 1978, Importance of apolar binding in complex-formation of cyclodextrins with adamantanecarboxylate, J Am Chem Soc, 100, 2259, 10.1021/ja00475a062
Kondo, 1993, Improved oral absorption of a poorly water-soluble drug, HO-221, by wet-bead milling producing particles in submicron region, Chem Pharm Bull (Tokyo), 41, 737, 10.1248/cpb.41.737
Konno, 2008, Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine, Eur J Pharm Biopharm, 70, 493, 10.1016/j.ejpb.2008.05.023
Konno, 2006, Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine, J Pharm Sci, 95, 2692, 10.1002/jps.20697
Konno, 2008, Ability of different polymers to inhibit the crystallization of amorphous felodipine in the presence of moisture, Pharm Res, 25, 969, 10.1007/s11095-007-9331-3
Kossena, 2003, Separation and characterization of the colloidal phases produced on digestion of common formulation lipids and assessment of their impact on the apparent solubility of selected poorly water-soluble drugs, J Pharm Sci, 92, 634, 10.1002/jps.10329
Kossena, 2004, Probing drug solubilization patterns in the gastrointestinal tract after administration of lipid-based delivery systems: a phase diagram approach, J Pharm Sci, 93, 332, 10.1002/jps.10554
Kossena, 2007, Low dose lipid formulations: effects on gastric emptying and biliary secretion, Pharm Res, 24, 2084, 10.1007/s11095-007-9363-8
Kostewicz, 2004, Predicting the precipitation of poorly soluble weak bases upon entry in the small intestine, J Pharm Pharmacol, 56, 43, 10.1211/0022357022511
Kou, 2011, In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC, Int J Pharm, 409, 75, 10.1016/j.ijpharm.2011.02.042
Kovács, 2009, Aqueous solvent system for the solubilization of azole compounds, Eur J Pharm Sci, 36, 352, 10.1016/j.ejps.2008.10.007
Kozlov, 2000, Relationship between pluronic block copolymer structure, critical micellization concentration and partitioning coefficients of low molecular mass solutes, Macromolecules, 33, 3305, 10.1021/ma991634x
Krauel-Goellner K (2008) Strategies to advance the bioavailability of low solubility drugs: increasing solubility using nanocrystals, in Controlled Release Society Annual Meeting, 2008 12–13 July, CRS Workshop, New York.
Krause, 2001, Production and characterisation of highly concentrated nanosuspensions by high pressure homogenisation, Int J Pharm, 214, 21, 10.1016/S0378-5173(00)00626-8
Krishna, 1989, Micellar solubilization of a new antimalarial drug, beta-arteether, J Pharm Sci, 78, 574, 10.1002/jps.2600780713
Kriwet, 1993, Binary diclofenac diethylamine water-systems: micelles, vesicles and lyotropic liquid-crystals, Eur J Pharm Biopharm, 39, 234
Krzyzaniak, 1997, Lysis of human red blood cells. 2. Effect of contact time on cosolvent induced hemolysis, Int J Pharm, 152, 193, 10.1016/S0378-5173(97)00082-3
Krzyzaniak, 1998, Lysis of human red blood cells. 3: Effect of contact time on surfactant-induced hemolysis, PDA J Pharm Sci Technol, 52, 66
Ku, 2010, Salt and polymorph selection strategy based on the Biopharmaceutical Classification System for early pharmaceutical development, Am Pharmaceutical Rev, 20, 30
Ku, 2010, Solutol HS15 as a novel excipient, Pharm Technol, 108, 110
Kumar, 2008, Preparation and characterization of salt forms of enalapril, Pharm Dev Technol, 13, 345, 10.1080/10837450802244686
Kumar L Amin A Bansal AK (2008b) Salt selection in drug development. Pharm Technol 3:128–146.
Kumar, 1999, Prechylomicron transport vesicle: isolation and partial characterization, Am J Physiol, 276, G378
Kurkov, 2011, Drug/cyclodextrin: beyond inclusion complexation, J Incl Phenom Macrocycl Chem, 69, 297, 10.1007/s10847-010-9756-x
Kwon, 2006, Amphiphilic block copolymer micelles for nanoscale drug delivery, Drug Dev Res, 67, 15, 10.1002/ddr.20063
Lai, 2009, Diclofenac nanosuspensions: influence of preparation procedure and crystal form on drug dissolution behaviour, Int J Pharm, 373, 124, 10.1016/j.ijpharm.2009.01.024
Lakshman, 2008, Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug, Mol Pharm, 5, 994, 10.1021/mp8001073
Langguth, 2005, Nanosuspension formulations for low-soluble drugs: pharmacokinetic evaluation using spironolactone as model compound, Drug Dev Ind Pharm, 31, 319, 10.1081/DDC-52182
Larsen, 2008, Lipid-based formulations for danazol containing a digestible surfactant, Labrafil M2125CS: in vivo bioavailability and dynamic in vitro lipolysis, Pharm Res, 25, 2769, 10.1007/s11095-008-9641-0
Larsen, 2009, Role of in vitro release models in formulation development and quality control of parenteral depots, Expert Opin Drug Deliv, 6, 1283, 10.1517/17425240903307431
Larsen, 2007, Diflunisal salts of bupivacaine, lidocaine and morphine: use of the common ion effect for prolonging the release of bupivacaine from mixed salt suspensions in an in vitro dialysis model, Eur J Pharm Sci, 31, 172, 10.1016/j.ejps.2007.03.005
Larson, 1986, Evaluation of supercritical fluid extraction in the pharmaceutical industry, Biotechnol Prog, 2, 73, 10.1002/btpr.5420020206
Lauer, 2011, Atomic force microscopy-based screening of drug-excipient miscibility and stability of solid dispersions, Pharm Res, 28, 572, 10.1007/s11095-010-0306-4
Laughlin RG (1994) The Aqueous Phase Behaviour of Surfactants, Academic Press, London.
Law, 2004, Ritonavir-PEG 8000 amorphous solid dispersions: in vitro and in vivo evaluations, J Pharm Sci, 93, 563, 10.1002/jps.10566
Law, 2002, Prediction of poly(ethylene) glycol-drug eutectic compositions using an index based on the van’t Hoff equation, Pharm Res, 19, 315, 10.1023/A:1014499119549
Law, 1992, Dissolution and absorption of nifedipine in polyethylene-glycol solid dispersion containing phosphatidylcholine, Int J Pharm, 84, 161, 10.1016/0378-5173(92)90056-8
Lawrence, 1994, Surfactant systems: their use in drug-delivery, Chem Soc Rev, 23, 417, 10.1039/cs9942300417
Ledwidge, 1998, Effects of surface active characteristics and solid state forms on the pH solubility profiles of drug-salt systems, Int J Pharm, 174, 187, 10.1016/S0378-5173(98)00257-9
Lee, 2009, Gefitinibcyclodextrin inclusion complexes: physico-chemical characterization and dissolution studies, Drug Dev Ind Pharm, 35, 1113, 10.1080/03639040902783074
Lespine, 2006, Contribution of lymphatic transport to the systemic exposure of orally administered moxidectin in conscious lymph duct-cannulated dogs, Eur J Pharm Sci, 27, 37, 10.1016/j.ejps.2005.08.003
Li-Blatter, 2009, Detergents as intrinsic P-glycoprotein substrates and inhibitors, Biochim Biophys Acta, 1788, 2335, 10.1016/j.bbamem.2009.07.010
Li, 2009, Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles, J Control Release, 133, 238, 10.1016/j.jconrel.2008.10.002
Li, 2009, Development of clinical dosage forms for a poorly water-soluble drug II: formulation and characterization of a novel solid microemulsion preconcentrate system for oral delivery of a poorly water-soluble drug, J Pharm Sci, 98, 1750, 10.1002/jps.21547
Li, 1999, Evaluation of intravenous flavopiridol formulations, PDA J Pharm Sci Technol, 53, 137
Li, 1999, Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants, J Pharm Sci, 88, 945, 10.1021/js990097r
Li, 1999, Combined effect of cosolvent and cyclodextrin on solubilization of nonpolar drugs, J Pharm Sci, 88, 1107, 10.1021/js990159d
Li, 2012, Enhanced bioavailability of a poorly water-soluble weakly basic compound using a combination approach of solubilization agents and precipitation inhibitors: a case study, Mol Pharm, 9, 1100, 10.1021/mp200352q
Li, 2005, Effect of chloride ion on dissolution of different salt forms of haloperidol, a model basic drug, J Pharm Sci, 94, 2224, 10.1002/jps.20440
Li, 2005, Investigation of solubility and dissolution of a free base and two different salt forms as a function of pH, Pharm Res, 22, 628, 10.1007/s11095-005-2504-z
Li, 2011, Development and in-vivo assessment of the bioavailability of oridonin solid dispersions by the gas anti-solvent technique, Int J Pharm, 411, 172, 10.1016/j.ijpharm.2011.04.006
Li, 2011, Preparation and in vitro/in vivo evaluation of revaprazan hydrochloride nanosuspension, Int J Pharm, 408, 157, 10.1016/j.ijpharm.2011.01.059
Li, 2011, Inhibition of lipase-catalyzed hydrolysis of emulsified triglyceride oils by low-molecular weight surfactants under simulated gastrointestinal conditions, Eur J Pharm Biopharm, 79, 423, 10.1016/j.ejpb.2011.03.019
Li, 1992, Induction of liver microsomal cytochrome P-450 2B1 by dimethyl diphenyl bicarboxylate in rats, Acta Pharmacol Sin, 13, 485
Liddle, 2008, The discovery of GSK221149A: a potent and selective oxytocin antagonist, Bioorg Med Chem Lett, 18, 90, 10.1016/j.bmcl.2007.11.008
Liedholm, 1986, Concomitant food intake can increase the bioavailability of propranolol by transient inhibition of its presystemic primary conjugation, Clin Pharmacol Ther, 40, 29, 10.1038/clpt.1986.135
Lima, 2011, The use of solid dispersion systems in hydrophilic carriers to increase benzonidazole solubility, J Pharm Sci, 100, 2443, 10.1002/jps.22436
Lin, 2011, Preclinical pharmacokinetic evaluation of resveratrol trimethyl ether in sprague-dawley rats: the impacts of aqueous solubility, dose escalation, food and repeated dosing on oral bioavailability, J Pharm Sci, 100, 4491, 10.1002/jps.22588
Lin, 1972, Preformulation investigation. I. Relation of salt forms and biological activity of an experimental antihypertensive, J Pharm Sci, 61, 1418, 10.1002/jps.2600610915
Lindfors, 2006, Amorphous drug nanosuspensions. 2. Experimental determination of bulk monomer concentrations, Langmuir, 22, 911, 10.1021/la052367t
Lindfors, 2008, Nucleation and crystal growth in supersaturated solutions of a model drug, J Colloid Interface Sci, 325, 404, 10.1016/j.jcis.2008.05.034
Lindman, 1980, Some aspects on the hydration of surfactant micelles, Pure Appl Chem, 52, 1307, 10.1351/pac198052051307
Lindmark, 1998, Absorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells, J Pharmacol Exp Ther, 284, 362
Linn, 2012, Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo, Eur J Pharm Sci, 45, 336, 10.1016/j.ejps.2011.11.025
Lipinski CA, Lombardo F, Dominy BW, and Feeney PJ (1997) Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 23:3–25.
List M and Sucker H (1988) inventors; Sandoz Ltd. Basel Switzerland, assignee. Pharmaceutical colloidal hydrosols for injection. GB Patent 2,200,048.
Liu, 2002, Dynamics of pharmaceutical amorphous solids: the study of enthalpy relaxation by isothermal microcalorimetry, J Pharm Sci, 91, 1853, 10.1002/jps.10181
Liu, 2002, The driving forces in the inclusion complexation of cyclodextrins, J Incl Phenom Macrocycl Chem, 42, 1, 10.1023/A:1014520830813
Liu, 2011, Nanosuspensions of poorly soluble drugs: preparation and development by wet milling, Int J Pharm, 411, 215, 10.1016/j.ijpharm.2011.03.050
Lloyd, 1997, An investigation into the melting behavior of binary mixes and solid dispersions of paracetamol and PEG 4000, J Pharm Sci, 86, 991, 10.1021/js970137w
Lo YL (2003) Relationships between the hydrophilic-lipophilic balance values of pharmaceutical excipients and their multidrug resistance modulating effect in Caco-2 cells and rat intestines. J Controlled Release 90:37–48.
Lockwood, 2003, Improved aqueous solubility of crystalline astaxanthin (3,3′-dihydroxy-beta, beta-carotene-4,4′-dione) by Captisol (sulfobutyl ether beta-cyclodextrin), J Pharm Sci, 92, 922, 10.1002/jps.10359
Loe, 1993, Interaction of multidrug-resistant Chinese hamster ovary cells with amphiphiles, Br J Cancer, 68, 342, 10.1038/bjc.1993.338
Loftsson, 2010, Pharmaceutical applications of cyclodextrins: basic science and product development, J Pharm Pharmacol, 62, 1607, 10.1111/j.2042-7158.2010.01030.x
Loftsson, 2011, Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes, J Pharm Pharmacol, 63, 1119, 10.1111/j.2042-7158.2011.01279.x
Loftsson, 1994, The effect of hydroxypropyl methylcellulose on the release of dexamethasone from aqueous 2-hydroxypropyl-beta-cyclodextrin formulations, Int J Pharm, 104, 181, 10.1016/0378-5173(94)90194-5
Loftsson, 2005, Evaluation of cyclodextrin solubilization of drugs, Int J Pharm, 302, 18, 10.1016/j.ijpharm.2005.05.042
Loftsson, 2007, The complexation efficiency, J Incl Phenom Macrocycl Chem, 57, 545, 10.1007/s10847-006-9247-2
Loftsson, 1993, Cyclodextrin complexation of NSAIDS: physicochemical characteristics, Eur J Pharm Sci, 1, 95, 10.1016/0928-0987(93)90023-4
Loftsson, 2007, Effects of cyclodextrins on drug delivery through biological membranes, J Pharm Sci, 96, 2532, 10.1002/jps.20992
Lohani S Grant DJW (2006) Thermodynamics of polymorphism, in Polymorphism in the Pharmaceutical Industry ( Hilfiker R ed) pp 21–42, WIiley-VCH, Weinheim, Germany.
Lohikangas, 1994, Effects of a new lipid-based drug-delivery system on the absorption of low-molecular-weight heparin (Fragmin) through monolayers of human intestinal epithelial Caco-2 Cells and after rectal administration to rabbits, Eur J Pharm Sci, 1, 297, 10.1016/0928-0987(94)90038-8
Lombardo, 1980, Studies on the substrate specificity of a carboxyl ester hydrolase from human pancreatic juice. I. Action on carboxyl esters, glycerides and phospholipids, Biochim Biophys Acta, 611, 136, 10.1016/0005-2744(80)90049-2
Longwell, 1976, Effect of topically applied pilocarpine on tear film pH, J Pharm Sci, 65, 1654, 10.1002/jps.2600651123
Lu, 1993, Dissolution modeling: factors affecting the dissolution rates of polydisperse powders, Pharm Res, 10, 1308, 10.1023/A:1018917729477
Lu, 2006, Characterization of a novel polymorphic form of celecoxib, J Pharm Sci, 95, 305, 10.1002/jps.20522
Lundin, 1997, Enhancing effects of monohexanoin and two other medium-chain glyceride vehicles on intestinal absorption of desmopressin (dDAVP), J Pharmacol Exp Ther, 282, 585
Luo, 2011, Pharmacokinetics, tissue distribution and relative bioavailability of puerarin solid lipid nanoparticles following oral administration, Int J Pharm, 410, 138, 10.1016/j.ijpharm.2011.02.064
Macie, 1986, Crystal-growth in pharmaceutical formulation, Pharm Int, 7, 233
Mackin, 2002, Quantification of low levels (<10%) of amorphous content in micronized active batches using dynamic vapour sorption and isothermal microcalorimetry, Int J Pharm, 231, 227, 10.1016/S0378-5173(01)00881-X
Madieh, 2007, Investigation of drug-porous adsorbent interactions in drug mixtures with selected porous adsorbents, J Pharm Sci, 96, 851, 10.1002/jps.20807
Magnusdottir, 2002, Self association and cyclodextrin solubilization of NSAIDs, J Incl Phenom Macrocycl Chem, 44, 213, 10.1023/A:1023079322024
Mahlin, 2011, Toward in silico prediction of glass-forming ability from molecular structure alone: a screening tool in early drug development, Mol Pharm, 8, 498, 10.1021/mp100339c
Majerik, 2007, Supercritical antisolvent versus coevaporation: preparation and characterization of solid dispersions, Drug Dev Ind Pharm, 33, 975, 10.1080/03639040601150286
Malcolmson, 1998, Effect of oil on the level of solubilization of testosterone propionate into nonionic oil-in-water microemulsions, J Pharm Sci, 87, 109, 10.1021/js9700863
Manca, 2005, Diclofenac-beta-cyclodextrin binary systems: physicochemical characterization and in vitro dissolution and diffusion studies, AAPS PharmSciTech, 6, E464, 10.1208/pt060358
Manjunath, 2006, Pharmacokinetics, tissue distribution and bioavailability of nitrendipine solid lipid nanoparticles after intravenous and intraduodenal administration, J Drug Target, 14, 632, 10.1080/10611860600888850
Manna, 2007, Impregnation of PVP microparticles with ketoprofen in the presence of supercritical CO2, J Supercrit Fluids, 42, 378, 10.1016/j.supflu.2006.12.002
Mansbach, 1991, Portal transport of absorbed lipids in rats, Am J Physiol, 261, G530
Mao, 2006, A calorimetric method to estimate molecular mobility of amorphous solids at relatively low temperatures, Pharm Res, 23, 2269, 10.1007/s11095-006-9071-9
Mao, 2006, Time-dependence of molecular mobility during structural relaxation and its impact on organic amorphous solids: an investigation based on a calorimetric approach, Pharm Res, 23, 1906, 10.1007/s11095-006-9008-3
Marsac, 2009, Estimation of drug-polymer miscibility and solubility in amorphous solid dispersions using experimentally determined interaction parameters, Pharm Res, 26, 139, 10.1007/s11095-008-9721-1
Marsac, 2008, Recrystallization of nifedipine and felodipine from amorphous molecular level solid dispersions containing poly(vinylpyrrolidone) and sorbed water, Pharm Res, 25, 647, 10.1007/s11095-007-9420-3
Marsac, 2006, A comparison of the physical stability of amorphous felodipine and nifedipine systems, Pharm Res, 23, 2306, 10.1007/s11095-006-9047-9
Masters K (1991) Spray Drying Handbook, Wiley, New York.
Matsumoto, 1999, Physical properties of solid molecular dispersions of indomethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinyl-acetate) in relation to indomethacin crystallization, Pharm Res, 16, 1722, 10.1023/A:1018906132279
Matteucci, 2007, Design of potent amorphous drug nanoparticles for rapid generation of highly supersaturated media, Mol Pharm, 4, 782, 10.1021/mp0700211
Mauludin, 2009, Development of an oral rutin nanocrystal formulation, Int J Pharm, 370, 202, 10.1016/j.ijpharm.2008.11.029
Maupas, 2011, Surfactant dependent toxicity of lipid nanocapsules in HaCaT cells, Int J Pharm, 411, 136, 10.1016/j.ijpharm.2011.03.056
Maurya, 2010, Microwave induced solubility enhancement of poorly water soluble atorvastatin calcium, J Pharm Pharmacol, 62, 1599, 10.1111/j.2042-7158.2010.01187.x
McClements, 2012, Crystals and crystallization in oil-in-water emulsions: implications for emulsion-based delivery systems, Adv Colloid Interface Sci, 174, 1, 10.1016/j.cis.2012.03.002
McGinity, 1984, Crystallinity and dissolution rate of tolbutamide solid dispersions prepared by the melt method, J Pharm Sci, 73, 1441, 10.1002/jps.2600731030
McIntosh, 2010, Impact of chlorpromazine self-association on its apparent binding constants with cyclodextrins: effect of SBE(7)-beta-CD on the disposition of chlorpromazine in the rat, J Pharm Sci, 99, 2999, 10.1002/jps.22064
McNamara, 1986, Dissolution of acidic and basic compounds from the rotating disk: influence of convective diffusion and reaction, J Pharm Sci, 75, 858, 10.1002/jps.2600750907
McNamara, 1988, Reaction plane approach for estimating the effects of buffers on the dissolution rate of acidic drugs, J Pharm Sci, 77, 511, 10.1002/jps.2600770610
McNamara, 2006, Use of a glutaric acid cocrystal to improve oral bioavailability of a low solubility API, Pharm Res, 23, 1888, 10.1007/s11095-006-9032-3
Meanwell, 1992, Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility, J Med Chem, 35, 2688, 10.1021/jm00092a020
Mehuys, 2005, Human bioavailability of propranolol from a matrix-in-cylinder system with a HPMC-Gelucire core, J Control Release, 107, 523, 10.1016/j.jconrel.2005.06.019
Mehuys, 2004, Hot-melt extruded ethylcellulose cylinders containing a HPMC-Gelucire core for sustained drug delivery, J Control Release, 94, 273, 10.1016/j.jconrel.2003.09.018
Mele, 1998, Non-covalent associations of cyclomaltooligosaccharides (cyclodextrins) with trans-beta-carotene in water: evidence for the formation of large aggregates by light scattering and NMR spectroscopy, Carbohydr Res, 310, 261, 10.1016/S0008-6215(98)00193-1
Mellaerts, 2007, Enhanced release of itraconazole from ordered mesoporous SBA-15 silica materials, Chem Commun (Camb), 13, 1375, 10.1039/b616746b
Mellaerts, 2008, Increasing the oral bioavailability of the poorly water soluble drug itraconazole with ordered mesoporous silica, Eur J Pharm Biopharm, 69, 223, 10.1016/j.ejpb.2007.11.006
Menegon, 2011, A nonstaining and tasteless hydrophobic salt of chlorhexidine, J Pharm Sci, 100, 3130, 10.1002/jps.22517
Menon, 2009, The assessment of human regional drug absorption of free acid and sodium salt forms of acipimox, in healthy volunteers, to direct modified release formulation strategy, Biopharm Drug Dispos, 30, 508, 10.1002/bdd.683
Merritt, 2007, Pharmacokinetics of dirlotapide in the dog, J Vet Pharmacol Ther, 30, 24, 10.1111/j.1365-2885.2007.00862.x
Messner, 2011, Self-assembly of cyclodextrins: the effect of the guest molecule, Int J Pharm, 408, 235, 10.1016/j.ijpharm.2011.02.008
Messner, 2010, Self-assembled cyclodextrin aggregates and nanoparticles, Int J Pharm, 387, 199, 10.1016/j.ijpharm.2009.11.035
Messner, 2011, Self-assembly of cyclodextrin complexes: effect of temperature, agitation and media composition on aggregation, Int J Pharm, 419, 322, 10.1016/j.ijpharm.2011.07.041
Miller, 2008, Enhanced in vivo absorption of itraconazole via stabilization of supersaturation following acidic-to-neutral pH transition, Drug Dev Ind Pharm, 34, 890, 10.1080/03639040801929273
Millward, 1998, Phase I trial of cremophor EL with bolus doxorubicin, Clin Cancer Res, 4, 2321
Miro, 2006, Drug/cyclodextrin solid systems in the design of hydrophilic matrices: a strategy to modulate drug delivery rate, Curr Drug Deliv, 3, 373, 10.2174/156720106778558994
Mishra, 2009, Production and characterization of hesperetin nanosuspensions for dermal delivery, Int J Pharm, 371, 182, 10.1016/j.ijpharm.2008.12.030
Mitra, 1982, Ophthalmic solution buffer systems. 1. The effect of buffer concentration on the ocular absorption of pilocarpine, Int J Pharm, 10, 219, 10.1016/0378-5173(82)90072-2
Miura, 2010, Enhancement of dissolution rate and oral absorption of a poorly water-soluble drug, K-832, by adsorption onto porous silica using supercritical carbon dioxide, Eur J Pharm Biopharm, 76, 215, 10.1016/j.ejpb.2010.06.016
Miyake, 2000, Improvement of solubility and oral bioavailability of rutin by complexation with 2-hydroxypropyl-beta-cyclodextrin, Pharm Dev Technol, 5, 399, 10.1081/PDT-100100556
Miyake, 1999, Enhanced absorption of cyclosporin A by complexation with dimethyl-beta-cyclodextrin in bile duct-cannulated and -noncannulated rats, Biol Pharm Bull, 22, 66, 10.1248/bpb.22.66
Miyake, 1999, Characterization of itraconazole/2-hydroxypropyl-beta-cyclodextrin inclusion complex in aqueous propylene glycol solution, Int J Pharm, 179, 237, 10.1016/S0378-5173(98)00393-7
Miyazaki, 1975, A comparison of solubility characteristics of free bases and hydrochloride salts of tetracycline antibiotics in hydrochloric acid solutions, Chem Pharm Bull (Tokyo), 23, 1197, 10.1248/cpb.23.1197
Miyazaki, 1980, Unusual solubility and dissolution behavior of pharmaceutical hydrochloride salts in chloride-containing media, Int J Pharm, 6, 77, 10.1016/0378-5173(80)90031-9
Miyazaki, 1981, Precaution on use of hydrochloride salts in pharmaceutical formulation, J Pharm Sci, 70, 594, 10.1002/jps.2600700604
Miyazaki, 2006, Physical stability of amorphous acetanilide derivatives improved by polymer excipients, Chem Pharm Bull (Tokyo), 54, 1207, 10.1248/cpb.54.1207
Miyazaki, 2007, Crystallization rate of amorphous nifedipine analogues unrelated to the glass transition temperature, Int J Pharm, 336, 191, 10.1016/j.ijpharm.2006.11.052
Miyazaki, 2004, Ability of polyvinylpyrrolidone and polyacrylic acid to inhibit the crystallization of amorphous acetaminophen, J Pharm Sci, 93, 2710, 10.1002/jps.20182
Moes, 2011, Pharmaceutical development and preliminary clinical testing of an oral solid dispersion formulation of docetaxel (ModraDoc001), Int J Pharm, 420, 244, 10.1016/j.ijpharm.2011.08.041
Mohamed, 2011, Computational prediction of salt and cocrystal structures: does a proton position matter?, Int J Pharm, 418, 187, 10.1016/j.ijpharm.2011.03.063
Mohsin, 2009, Design of lipid-based formulations for oral administration of poorly water-soluble drugs: precipitation of drug after dispersion of formulations in aqueous solution, J Pharm Sci, 98, 3582, 10.1002/jps.21659
Moneghini, 2010, Characterization of solid dispersions of itraconazole and vitamin E TPGS prepared by microwave technology, Future Med Chem, 2, 237, 10.4155/fmc.09.166
Moneghini, 2001, Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterisation, and in vitro dissolution, Int J Pharm, 222, 129, 10.1016/S0378-5173(01)00711-6
Moneghini, 2009, Influence of the microwave technology on the physical-chemical properties of solid dispersion with nimesulide, Powder Technol, 195, 259, 10.1016/j.powtec.2009.06.006
Monkhouse, 1972, Use of adsorbents in enhancement of drug dissolution. I, J Pharm Sci, 61, 1430, 10.1002/jps.2600610917
Monkhouse, 1972, Use of adsorbents in enhancement of drug dissolution. II, J Pharm Sci, 61, 1435, 10.1002/jps.2600610918
Mooney, 1981, Dissolution kinetics of carboxylic acids I. effect of pH under unbuffered conditions, J Pharm Sci, 70, 13, 10.1002/jps.2600700103
Moribe, 2005, Micronization of phenylbutazone by rapid expansion of supercritical CO2 solution, Chem Pharm Bull (Tokyo), 53, 1025, 10.1248/cpb.53.1025
Morris, 1988, Solubility of aromatic pollutants in mixed-solvents, Chemosphere, 17, 285, 10.1016/0045-6535(88)90221-4
Morris, 1994, An integrated approach to the selection of optimal salt form for a new drug candidate, Int J Pharm, 105, 209, 10.1016/0378-5173(94)90104-X
Morris, 2001, Theoretical approaches to physical transformations of active pharmaceutical ingredients during manufacturing processes, Adv Drug Deliv Rev, 48, 91, 10.1016/S0169-409X(01)00100-4
Morris, 1992, Structural properties of polyethylene glycol-polysorbate 80 mixture, a solid dispersion vehicle, J Pharm Sci, 81, 1185, 10.1002/jps.2600811212
Möschwitzer, 2004, Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology, Eur J Pharm Biopharm, 58, 615, 10.1016/j.ejpb.2004.03.022
Mosharraf, 1995, The effect of particle-size and shape on the surface specific dissolution rate of microsized practically insoluble drugs, Int J Pharm, 122, 35, 10.1016/0378-5173(95)00033-F
Mottu, 2000, Organic solvents for pharmaceutical parenterals and embolic liquids: a review of toxicity data, PDA J Pharm Sci Technol, 54, 456
Mountfield, 2000, Potential inhibitory effects of formulation ingredients on intestinal cytochrome P450, Int J Pharm, 211, 89, 10.1016/S0378-5173(00)00586-X
Mudra, 2010, Absorption barriers in the rat intestinal mucosa. 3. Effects of polyethoxylated solubilizing agents on drug permeation and metabolism, J Pharm Sci, 99, 1016, 10.1002/jps.21836
Mueller, 1994, Minor influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporine, Transplant Proc, 26, 2957
Mueller, 1994, Influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporine in a crossover comparison with the market formulation, Pharm Res, 11, 151, 10.1023/A:1018922517162
Muhrer, 2006, Use of compressed gas precipitation to enhance the dissolution behavior of a poorly water-soluble drug: generation of drug microparticles and drug-polymer solid dispersions, Int J Pharm, 308, 69, 10.1016/j.ijpharm.2005.10.026
Mukerjee P (1979) Solubilization in aqueous micellar micelles, in Solution Chemistry of Surfactants ( Mittal KL ed) pp 153–174, Plenum Press, New York.
Muller RH Becker R Kruss B Peters K (1999), inventors Medac Gesellschafft Fur Klinische Spezialpraparate, Hamburg, Germany, assignee. Pharmaceutical nanosuspensions for medicament administration as systems with increases saturation solubility and rate of solution. U.S. Patent, 5,858,410.
Müller RH Bohm BHL (1998) Nanosuspensions, in Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs ( Muller RH Benita S Bohm B eds) pp 149–174, Medpharm, Stuttgart, Germany.
Müller RH Junghanns JAW (1998) Drug nanocrystals/nanosuspensions for the delivery of poorly soluble drugs, in Nanoparticulates as drug carriers ( Torchilin VP ed) pp 307–328, Imperial College Press London.
Müller, 2011, 20 years of lipid nanoparticles (SLN and NLC): present state of development and industrial applications, Curr Drug Discov Technol, 8, 207, 10.2174/157016311796799062
Müllertz, 2012, Insights into intermediate phases of human intestinal fluids visualized by atomic force microscopy and cryo-transmission electron microscopy ex vivo, Mol Pharm, 9, 237, 10.1021/mp200286x
Müllertz, 2010, New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs, J Pharm Pharmacol, 62, 1622, 10.1111/j.2042-7158.2010.01107.x
Mura, 1999, Effects of the host cavity size and the preparation method on the physicochemical properties of ibuproxam-cyclodextrin systems, Drug Dev Ind Pharm, 25, 279, 10.1081/DDC-100102172
Mura, 2005, Solid-state characterization and dissolution properties of naproxen-arginine-hydroxypropyl-beta-cyclodextrin ternary system, Eur J Pharm Biopharm, 59, 99, 10.1016/j.ejpb.2004.05.005
Mura, 1998, Interactions of ketoprofen and ibuprofen with beta-cyclodextrins in solution and in the solid state, Int J Pharm, 166, 189, 10.1016/S0378-5173(98)00035-0
Mura, 2001, The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin, Eur J Pharm Sci, 13, 187, 10.1016/S0928-0987(01)00093-8
Mura, 2001, Multicomponent systems of econazole with hydroxyacids and cyclodextrins, J Incl Phenom Macrocycl Chem, 39, 131, 10.1023/A:1008114411503
Murdam S Florence AT (2000) Non-aqueous solutions and suspensions as sustained-release injectable formulations, in Sustained-Release Injectable Products ( Senior J Radomsky M eds) pp 71–107, Interpharm Press, Denver, CO.
Murdande, 2010, Solubility advantage of amorphous pharmaceuticals: I. A thermodynamic analysis, J Pharm Sci, 99, 1254, 10.1002/jps.21903
Murdande, 2010, Solubility advantage of amorphous pharmaceuticals: II. Application of quantitative thermodynamic relationships for prediction of solubility enhancement in structurally diverse insoluble pharmaceuticals, Pharm Res, 27, 2704, 10.1007/s11095-010-0269-5
Murdande, 2011, Aqueous solubility of crystalline and amorphous drugs: challenges in measurement, Pharm Dev Technol, 16, 187, 10.3109/10837451003774377
Murdande, 2011, Solubility advantage of amorphous pharmaceuticals. III. Is maximum solubility advantage experimentally attainable and sustainable?, J Pharm Sci, 100, 4349, 10.1002/jps.22643
Myers, 1992, Systemic bioavailability of penclomedine (NSC-338720) from oil-in-water emulsions administered intraduodenally to rats, Int J Pharm, 78, 217, 10.1016/0378-5173(92)90374-B
Myers, 1993, Solid-state emulsions: the effects of maltodextrin on microcrystalline aging, Pharm Res, 10, 1389, 10.1023/A:1018998519907
Na, 1999, Cloud point of nonionic surfactants: modulation with pharmaceutical excipients, Pharm Res, 16, 562, 10.1023/A:1018831415131
Nagapudi, 2008, Amorphous active pharmaceutical ingredients in preclinical studies, Current Bioactive Compounds, 4, 213, 10.2174/157340708786847852
Nagarsenker, 2000, Solid dispersion of hydroxypropyl beta-cyclodextrin and ketorolac: enhancement of in-vitro dissolution rates, improvement in anti-inflammatory activity and reduction in ulcerogenicity in rats, J Pharm Pharmacol, 52, 949, 10.1211/0022357001774831
Nakach, 2004, Comparison of various milling technologies for grinding pharmaceutical powders, Int J Miner Process, 74, S173, 10.1016/j.minpro.2004.07.039
Nakai, 1990, Study of the interaction of clobazam with cyclodextrins in solution and in the solid state, Chem Pharm Bull (Tokyo), 38, 728, 10.1248/cpb.38.728
Nakanishi, 1989, Effect of the interaction of drug-beta-cyclodextrin complex with bile salts on the drug absorption from rat small intestinal lumen, Chem Pharm Bull (Tokyo), 37, 211, 10.1248/cpb.37.211
Nambu, 1978, Bioavailability of powdered inclusion compounds of nonsteroidal anti-inflammatory drugs with β−cyclodextrin in rabbits and dogs, Chem Pharm Bull (Tokyo), 26, 2952, 10.1248/cpb.26.2952
Nandi, 2003, Synergistic effect of PEG-400 and cyclodextrin to enhance solubility of progesterone, AAPS PharmSciTech, 4, E1, 10.1208/pt040101
Narazaki, 2007, Estimation of drug precipitation upon dilution of pH-controlled formulations, Mol Pharm, 4, 550, 10.1021/mp070007o
Narazaki, 2007, Estimation of drug precipitation upon dilution of pH-cosolvent solubilized formulations, Chem Pharm Bull (Tokyo), 55, 1203, 10.1248/cpb.55.1203
Nassar, 2004, Influence of formaldehyde impurity in polysorbate 80 and PEG-300 on the stability of a parenteral formulation of BMS-204352: identification and control of the degradation product, Pharm Dev Technol, 9, 189, 10.1081/PDT-120030249
Neervannan, 2006, Preclinical formulations for discovery and toxicology: physicochemical challenges, Expert Opin Drug Metab Toxicol, 2, 715, 10.1517/17425255.2.5.715
Nehm, 2006, Phase solubility diagrams of cocrystals are explained by solubility product and solution complexation, Cryst Growth Des, 6, 592, 10.1021/cg0503346
Nekkanti, 2009, Development and characterization of solid oral dosage form incorporating candesartan nanoparticles, Pharm Dev Technol, 14, 290, 10.1080/10837450802585278
Nelson, 1957, Solution rate of theophylline salts and effects from oral administration, J Pharm Sci, 46, 607, 10.1002/jps.3030461012
Nema, 1997, Excipients and their use in injectable products, PDA J Pharm Sci Technol, 51, 166
Newman, 2012, Assessing the performance of amorphous solid dispersions, J Pharm Sci, 101, 1355, 10.1002/jps.23031
Ngai, 1998, Correlation between the secondary beta-relaxation time at Tg with the Kohlrausch exponent of the primary alpha relaxation or the fragility of glass-forming materials, Phys Rev E, 57, 7346, 10.1103/PhysRevE.57.7346
Ngai, 2010, Recent progress in understanding relaxation in complex systems, J Non-Cryst Solids, 356, 535, 10.1016/j.jnoncrysol.2009.03.011
Ngai, 2001, Nature and properties of the Johari-Goldstein beta-relaxation in the equilibrium liquid state of a class of glass-formers, J Chem Phys, 115, 1405, 10.1063/1.1381054
Nguyen, 2010, Phytantriol and glyceryl monooleate cubic liquid crystalline phases as sustained-release oral drug delivery systems for poorly water-soluble drugs. II. In-vivo evaluation, J Pharm Pharmacol, 62, 856, 10.1211/jpp.62.07.0006
Ni, 2002, Solubilization and preformulation of carbendazim, Int J Pharm, 244, 99, 10.1016/S0378-5173(02)00318-6
Nicklasson, 1984, The relationship between intrinsic dissolution rates and solubilities in the water ethanol binary solvent system, Int J Pharm, 18, 149, 10.1016/0378-5173(84)90115-7
Nicklasson, 1981, Studies on the relationship between solubility and intrinsic rate of dissolution as a function of pH, Acta Pharm Suec, 18, 119
Nicolaides, 2001, Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration, Pharm Res, 18, 380, 10.1023/A:1011071401306
Nielloud F Marti-Mestres G (2000) Pharmaceutical Emulsions and Suspensions, Marcel Dekker Inc, Basel, Switzerland.
Nimmerfall, 1980, Dependence of area under the curve on proquazone particle size and in vitro dissolution rate, J Pharm Sci, 69, 605, 10.1002/jps.2600690538
Niot I Besnard P (2004) Intestinal fat absorption: roles of intracellular lipid-binding proteins and peroxisome proliferator-activated receptors, in Cellular Proteins and Their Fatty Acids in Health and Disease pp 359–381, Wiley-VCH, Weinheim, Germany.
Nishino M Enachescu C Miyashita S Rikvold PA Boukheddaden K Varret F (2011) Macroscopic nucleation phenomena in continuum media with long-range interactions. Scientific Reports 1 DOI: 10.1038/srep00162.
Niwa, 2011, Design of dry nanosuspension with highly spontaneous dispersible characteristics to develop solubilized formulation for poorly water-soluble drugs, Pharm Res, 28, 2339, 10.1007/s11095-011-0465-y
Niwa, 2011, Universal wet-milling technique to prepare oral nanosuspension focused on discovery and preclinical animal studies: development of particle design method, Int J Pharm, 405, 218, 10.1016/j.ijpharm.2010.12.013
Nokhodchi, 2003, Crystal modification of phenytoin using different solvents and crystallization conditions, Int J Pharm, 250, 85, 10.1016/S0378-5173(02)00488-X
Nykamp, 2002, Jet milling: a new technique for microparticle preparation, Int J Pharm, 242, 79, 10.1016/S0378-5173(02)00150-3
Nystrom C (1998) Dissolution properties of poorly soluble drugs: Theoretical background and possibilities to improve dissolution behaviour, in Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs ( Muller RH Benita S Bohm B eds) pp 143–148, Medpharm, Stuttgart, Germany.
O’Connor, 2001, Preparation and characterisation of a range of diclofenac salts, Int J Pharm, 226, 163, 10.1016/S0378-5173(01)00800-6
Offerdahl, 2005, Quantitation of crystalline and amorphous forms of anhydrous neotame using 13C CPMAS NMR spectroscopy, J Pharm Sci, 94, 2591, 10.1002/jps.20469
Oh, 2011, Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier, Int J Pharm, 420, 412, 10.1016/j.ijpharm.2011.09.007
Ohara, 2005, Dissolution mechanism of poorly water-soluble drug from extended release solid dispersion system with ethylcellulose and hydroxypropylmethylcellulose, Int J Pharm, 302, 95, 10.1016/j.ijpharm.2005.06.019
Ohgaki, 1992, Heterogeneity in aqueous-solutions: electron-microscopy of citric-acid solutions, Chem Eng Sci, 47, 1819, 10.1016/0009-2509(92)80300-2
Okimoto, 1997, Dissolution mechanism and rate of solid dispersion particles of nilvadipine with hydroxypropylmethylcellulose, Int J Pharm, 159, 85, 10.1016/S0378-5173(97)00274-3
Okimoto, 1999, Release of testosterone from an osmotic pump tablet utilizing (SBE)7m-beta-cyclodextrin as both a solubilizing and an osmotic pump agent, J Control Release, 58, 29, 10.1016/S0168-3659(98)00142-4
Okonogi, 1997, Improved dissolution of ofloxacin via solid dispersion, Int J Pharm, 156, 175, 10.1016/S0378-5173(97)00196-8
Oliveira, 1993, Cholesteryl esters in lymph chylomicrons: contribution from high density lipoprotein transferred from plasma into intestinal lymph, J Lipid Res, 34, 1729, 10.1016/S0022-2275(20)35735-7
Omar, 2007, Inclusion complexation of loratadine with natural and modified cyclodextrins: phase solubility and thermodynamic studies, J Solution Chem, 36, 605, 10.1007/s10953-007-9136-3
Ong, 1988, Micellar solubilization of timobesone acetate in aqueous and aqueous propylene glycol solutions of nonionic surfactants, Pharm Res, 5, 704, 10.1023/A:1015903827042
Onizuka, 1997, Lymph flow pattern in the intact thoracic duct in sheep, J Physiol, 503, 223, 10.1111/j.1469-7793.1997.223bi.x
Orlowski, 1998, Effects of detergents on P-glycoprotein atpase activity: differences in perturbations of basal and verapamil-dependent activities, Cancer Biochem Biophys, 16, 85
Orsenigo, 1990, Characterization of basolateral membrane Na/H antiport in rat jejunum, Biochim Biophys Acta, 1026, 64, 10.1016/0005-2736(90)90333-J
Oteroespinar, 1991, Oral bioavailability of naproxen-beta-cyclodextrin inclusion compound, Int J Pharm, 75, 37, 10.1016/0378-5173(91)90248-M
Otsuka, 1993, Hygroscopic stability and dissolution properties of spray-dried solid dispersions of furosemide with Eudragit, J Pharm Sci, 82, 32, 10.1002/jps.2600820108
Ozaki, 2012, Supersaturation-nucleation behavior of poorly soluble drugs and its impact on the oral absorption of drugs in thermodynamically high-energy forms, J Pharm Sci, 101, 214, 10.1002/jps.22760
Padden B Miller JM Robbins T Zocharski PD Prasad L Spence JK LaFountaine J (2011) Amorphous solid dispersions as enabling formulations for discovery and early development. Am Pharm Rev 1:66–73.
Padrela, 2009, Formation of indomethacin-saccharin cocrystals using supercritical fluid technology, Eur J Pharm Sci, 38, 9, 10.1016/j.ejps.2009.05.010
Pajula, 2010, Predicting the formation and stability of amorphous small molecule binary mixtures from computationally determined Flory-Huggins interaction parameter and phase diagram, Mol Pharm, 7, 795, 10.1021/mp900304p
Palin, 1984, The effect of different oils on the absorption of probucol in the rat, J Pharm Pharmacol, 36, 641, 10.1111/j.2042-7158.1984.tb04919.x
Palucki, 2010, Strategies at the interface of drug discovery and development: early optimization of the solid state phase and preclinical toxicology formulation for potential drug candidates, J Med Chem, 53, 5897, 10.1021/jm1002638
Pan, 1996, Enhanced oral cyclosporine absorption with water-soluble vitamin E early after liver transplantation, Pharmacotherapy, 16, 59, 10.1002/j.1875-9114.1996.tb02916.x
Pan, 2008, Increasing the dissolution rate of a low-solubility drug through a crystalline-amorphous transition: a case study with indomethicin, Drug Dev Ind Pharm, 34, 221, 10.1080/03639040701580606
Pandit, 1984, Effect of crystal form on the oral absorption of phenylbutazone, Int J Pharm, 21, 129, 10.1016/0378-5173(84)90210-2
Papadimitriou, 2008, Microwave-induced enhancement of the dissolution rate of poorly water-soluble tibolone from poly(ethylene glycol) solid dispersions, J Appl Polym Sci, 108, 1249, 10.1002/app.27746
Papp, 1962, An electron microscopic study of the central lacteal in the intestinal villus of the cat, Z Zellforsch Mikrosk Anat, 57, 475, 10.1007/BF00339877
Pardeike, 2009, Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products, Int J Pharm, 366, 170, 10.1016/j.ijpharm.2008.10.003
Pardeike, 2010, Nanosuspensions: a promising formulation for the new phospholipase A2 inhibitor PX-18, Int J Pharm, 391, 322, 10.1016/j.ijpharm.2010.03.002
Park, 1989, Association of anionic surfactants with beta-cyclodextrin: fluorescence-probed studies on the 1-1 and 1-2 complexation, J Phys Chem, 93, 6454, 10.1021/j100354a035
Parshad, 2002, Correlation of aqueous solubility of salts of benzylamine with experimentally and theoretically derived parameters: a multivariate data analysis approach, Int J Pharm, 237, 193, 10.1016/S0378-5173(02)00042-X
Parshad, 2004, Aqueous solubility study of salts of benzylamine derivatives and p-substituted benzoic acid derivatives using X-ray crystallographic analysis, Int J Pharm, 269, 157, 10.1016/j.ijpharm.2003.09.009
Partyka M Au BH Evans CH (2001) Cyclodextrins as phototoxicity inhibitors in drug formulations: studies on model systems involving naproxen and beta-cyclodextrin. J Photochem Photobiol a. Chemistry 140:67–74.
Paruta, 1964, Solubility of salicylic acid as a function of dielectric constant, J Pharm Sci, 53, 1349, 10.1002/jps.2600531114
Pasquali, 2006, Solid-state chemistry and particle engineering with supercritical fluids in pharmaceutics, Eur J Pharm Sci, 27, 299, 10.1016/j.ejps.2005.11.007
Passerini, 2006, Evaluation of melt granulation and ultrasonic spray congealing as techniques to enhance the dissolution of praziquantel, Int J Pharm, 318, 92, 10.1016/j.ijpharm.2006.03.028
Patel, 2006, Effect of hydrophilic polymer on solubilization of fenofibrate by cyclodextrin complexation, J Incl Phenom Macrocycl Chem, 56, 247, 10.1007/s10847-006-9091-4
Patel, 2009, The effect of oral lipids and circulating lipoproteins on the metabolism of drugs, Expert Opin Drug Metab Toxicol, 5, 1385, 10.1517/17425250903176439
Patel, 2010, Effect of bile and lipids on the stereoselective metabolism of halofantrine by rat everted-intestinal sacs, Chirality, 22, 275, 10.1002/chir.20740
Patil, 2006, Porous polystyrene beads as carriers for self-emulsifying system containing loratadine, AAPS PharmSciTech, 7, E28, 10.1208/pt070128
Patt, 1999, Butenolide endothelin antagonists with improved aqueous solubility, J Med Chem, 42, 2162, 10.1021/jm980504w
Patterson, 2008, Melt extrusion and spray drying of carbamazepine and dipyridamole with polyvinylpyrrolidone/vinyl acetate copolymers, Drug Dev Ind Pharm, 34, 95, 10.1080/03639040701484627
Patton, 1984, The light microscopy of triglyceride digestion, Food Microstruct, 4, 29
Paudel, 2010, Theoretical and experimental investigation on the solid solubility and miscibility of naproxen in poly(vinylpyrrolidone), Mol Pharm, 7, 1133, 10.1021/mp100013p
Paulekuhn, 2007, Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database, J Med Chem, 50, 6665, 10.1021/jm701032y
Pedersen, 1997, The bioavailability difference between genuine cyclodextrin inclusion complexes and freeze-dried or ground drug cyclodextrin samples may be due to supersaturation differences, Drug Dev Ind Pharm, 23, 331, 10.3109/03639049709149812
Pedersen, 1993, Formation and antimycotic effect of cyclodextrin inclusion complexes of econazole and miconazole, Int J Pharm, 90, 247, 10.1016/0378-5173(93)90197-N
Peltonen, 2010, Pharmaceutical nanocrystals by nanomilling: critical process parameters, particle fracturing and stabilization methods, J Pharm Pharmacol, 62, 1569, 10.1111/j.2042-7158.2010.01022.x
Perng, 2003, Assessment of oral bioavailability enhancing approaches for SB-247083 using flow-through cell dissolution testing as one of the screens, Int J Pharm, 250, 147, 10.1016/S0378-5173(02)00521-5
Peterson ML Collier EA Hickey MB Guzman H Almarsson O (2010) Multi-component pharmaceutical crystalline phases: engineering for performance, in Organic Crystal Engineering: Frontiers in Crystal Engineering ( Tiekink ERT Vittal J Zaworotko MJ eds) Wiley, New York.
Lee, 2009, Gefitinib-cyclodextrin inclusion complexes: physico-chemical characterization and dissolution studies, Drug Dev Ind Pharm, 35, 1113, 10.1080/03639040902783074
Phillips, 1993, Rapid expansion from supercritical solutions: application to pharmaceutical processes, Int J Pharm, 94, 1, 10.1016/0378-5173(93)90002-W
Piel, 1998, Development of a non-surfactant parenteral formulation of miconazole by the use of cyclodextrins, Int J Pharm, 169, 15, 10.1016/S0378-5173(98)00103-3
Plakkot, 2011, Comminution of ibuprofen to produce nano-particles for rapid dissolution, Int J Pharm, 415, 307, 10.1016/j.ijpharm.2011.06.002
Pole, 2008, Physical and biological considerations for the use of nonaqueous solvents in oral bioavailability enhancement, J Pharm Sci, 97, 1071, 10.1002/jps.21060
*Porter CJH, Charman SA, Williams RD, Bakalova MV, and Charman WN (1996) Evaluation of emulsifiable glasses for the oral administration of cyclosporin in beagle dogs. Int J Pharm 141:227–237.
Porter CJH Anby MU Warren DB Williams HD Benameur H Pouton CW (2011) Lipid based formulations: exploring the link between in vitro supersaturation and in vivo exposure. Bull Tech Gattefosse 104:61–69.
Porter, 2004, Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine, J Pharm Sci, 93, 1110, 10.1002/jps.20039
Porter, 2008, Lipid-based systems for the enhanced delivery of poorly water soluble drugs, Adv Drug Deliv Rev, 60, 615, 10.1016/j.addr.2007.10.009
Pouton, 2000, Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems, Eur J Pharm Sci, 11, S93, 10.1016/S0928-0987(00)00167-6
Pralhad, 2004, Study of freeze-dried quercetin-cyclodextrin binary systems by DSC, FT-IR, X-ray diffraction and SEM analysis, J Pharm Biomed Anal, 34, 333, 10.1016/S0731-7085(03)00529-6
Preté, 2002, Solubilization of human erythrocyte membranes by non-ionic surfactants of the polyoxyethylene alkyl ethers series, Biophys Chem, 97, 45, 10.1016/S0301-4622(02)00042-X
Prevosto, 2009, Does the entropy and volume dependence of the structural alpha-relaxation originate from the Johari-Goldstein beta-relaxation?, J Non-Cryst Solids, 355, 705, 10.1016/j.jnoncrysol.2008.09.043
Prevosto, 2008, Relationship between structural and secondary relaxation in glass formers: Ratio between glass transition temperature and activation energy, Philos Mag, 88, 4063, 10.1080/14786430802389205
Pudipeddi M Serajuddin ATM Grant DJW Stahl PH (2002) Solubility and dissolution of weak acids, bases and salts, in Handbook of Pharmaceutical Salts: Properties, Selection and Use (Stahl PH and Wermuth GH eds) pp 19–40, Wiley-VCH, Weinheim, Germany.
Qi S Craig DQM (2010) Detection of phase separation in hot melt extruded solid dispersion formulations. Am Pharm Rev 68–74.
Qian, 2010, Drug-polymer solubility and miscibility: stability consideration and practical challenges in amorphous solid dispersion development, J Pharm Sci, 99, 2941, 10.1002/jps.22074
Qian, 2010, Is a distinctive single Tg a reliable indicator for the homogeneity of amorphous solid dispersion?, Int J Pharm, 395, 232, 10.1016/j.ijpharm.2010.05.033
Qian, 2011, Spontaneous crystalline-to-amorphous phase transformation of organic or medicinal compounds in the presence of porous media, part 1: thermodynamics of spontaneous amorphization, J Pharm Sci, 100, 2801, 10.1002/jps.22519
Qian, 2012, Application of mesoporous silicon dioxide and silicate in oral amorphous drug delivery systems, J Pharm Sci, 101, 444, 10.1002/jps.22779
Qian, 2011, Spontaneous crystalline-to-amorphous phase transformation of organic or medicinal compounds in the presence of porous media. Part 2. Amorphization capacity and mechanisms of interaction, J Pharm Sci, 100, 4674, 10.1002/jps.22657
Qiao, 2011, Pharmaceutical cocrystals: an overview, Int J Pharm, 419, 1, 10.1016/j.ijpharm.2011.07.037
Quintão, 1979, Origin of cholesterol transported in intestinal lymph: studies in patients with filarial chyluria, J Lipid Res, 20, 941, 10.1016/S0022-2275(20)39995-8
Rabinow, 2007, Itraconazole IV nanosuspension enhances efficacy through altered pharmacokinetics in the rat, Int J Pharm, 339, 251, 10.1016/j.ijpharm.2007.02.030
Raghavan, 1996, Solubility enhancement of a bisnaphthalimide tumoricidal agent, DMP 840, through complexation, Pharm Dev Technol, 1, 231, 10.3109/10837459609022591
Raghavan, 2001, Crystallization of hydrocortisone acetate: influence of polymers, Int J Pharm, 212, 213, 10.1016/S0378-5173(00)00610-4
Rama Prasad, 2003, Evaluation of oral formulations of gentamicin containing labrasol in beagle dogs, Int J Pharm, 268, 13, 10.1016/j.ijpharm.2003.08.008
Rama Prasad, 2004, In situ intestinal absorption studies on low molecular weight heparin in rats using labrasol as absorption enhancer, Int J Pharm, 271, 225, 10.1016/j.ijpharm.2003.11.013
Ran, 2005, Solubilization and preformulation studies on PG-300995 (an anti-HIV drug), J Pharm Sci, 94, 297, 10.1002/jps.20246
Randall, 2011, Evaluation of surfactants as solubilizing agents in microsomal metabolism reactions with lipophilic substrates, Vitro Cell Dev Biol Anim, 47, 631, 10.1007/s11626-011-9449-9
Rangel-Yagui, 2005, Micellar solubilization of drugs, J Pharm Pharm Sci, 8, 147
Rao, 2001, Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl methylcellulose matrix tablets using (SBE)(7m)-beta-cyclodextrin as a solubilizing agent, J Pharm Sci, 90, 807, 10.1002/jps.1034
Rao, 2006, Co-solubilization of poorly soluble drugs by micellization and complexation, Int J Pharm, 319, 98, 10.1016/j.ijpharm.2006.03.042
Rao, 2010, Inhibitive effect of cremophor RH40 or tween 80-based self-microemulsiflying drug delivery system on cytochrome P450 3A enzymes in murine hepatocytes, J Huazhong Univ Sci Technolog Med Sci, 30, 562, 10.1007/s11596-010-0543-0
Rasenack, 2002, Dissolution rate enhancement by in situ micronization of poorly water-soluble drugs, Pharm Res, 19, 1894, 10.1023/A:1021410028371
Redenti, 2000, Drug/cyclodextrin/hydroxy acid multicomponent systems: properties and pharmaceutical applications, J Pharm Sci, 89, 1, 10.1002/(SICI)1520-6017(200001)89:1<1::AID-JPS1>3.0.CO;2-W
Reed, 1985, Lysis of human red blood cells in the presence of various cosolvents, J Parenter Sci Technol, 39, 64
Reed, 1986, Lysis of human red blood cells in the presence of various cosolvents. II. The effect of differing NaCl concentrations, J Parenter Sci Technol, 40, 88
Reer, 1993, Investigation of the influence of cosolvents and surfactants on the complexation of dexamethasone with hydroxypropyl-beta-cyclodextrin by use of a simplex lattice design, Eur J Pharm Biopharm, 39, 105
Rege BD Kao JP Polli JE (2002) Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur J Pharm Sci 16:237–246.
Regev, 1999, Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells, Eur J Biochem, 259, 18, 10.1046/j.1432-1327.1999.00037.x
Remenar, 2003, Crystal engineering of novel cocrystals of a triazole drug with 1,4-dicarboxylic acids, J Am Chem Soc, 125, 8456, 10.1021/ja035776p
Remenar, 2007, Celecoxib:nicotinamide dissociation: using excipients to capture the cocrystal’s potential, Mol Pharm, 4, 386, 10.1021/mp0700108
Ren X Mao X Cao L Xue K Si L Qiu J Schimmer AD Li G (2009) Nonionic surfactants are strong inhibitors of cytochrome P450 3A biotransformation activity in vitro and in vivo. Eur J Pharm Sci 36:401–411.
Repka, 2007, Pharmaceutical applications of hot-melt extrusion: Part II, Drug Dev Ind Pharm, 33, 1043, 10.1080/03639040701525627
Reppas, 1991, Effect of hydroxypropylmethylcellulose on gastrointestinal transit and luminal viscosity in dogs, Gastroenterology, 100, 1217, 10.1016/0016-5085(91)70007-K
Reverchon, 2002, Rifampicin microparticles production by supercritical antisolvent precipitation, Int J Pharm, 243, 83, 10.1016/S0378-5173(02)00261-2
Reverchon, 2007, Nanoparticles production by supercritical antisolvent precipitation: a general interpretation, J Supercrit Fluids, 43, 126, 10.1016/j.supflu.2007.04.013
Ribeiro, 2008, Preparation and solid-state characterization of inclusion complexes formed between miconazole and methyl-beta-cyclodextrin, AAPS PharmSciTech, 9, 1102, 10.1208/s12249-008-9143-8
Ribeiro Dos Santos, 2003, A supercritical fluid-based coating technology. 2: solubility considerations, J Microencapsul, 20, 97, 10.1080/02652040210162649
Ribeiro, 2005, Multicomponent complex formation between vinpocetine, cyclodextrins, tartaric acid and water-soluble polymers monitored by NMR and solubility studies, Eur J Pharm Sci, 24, 1, 10.1016/j.ejps.2004.09.003
Ribeiro, 2005, In vitro controlled release of vinpocetine-cyclodextrin-tartaric acid multicomponent complexes from HPMC swellable tablets, J Control Release, 103, 325, 10.1016/j.jconrel.2004.12.001
Ribeiro, 2003, Investigation and physicochemical characterization of vinpocetine-sulfobutyl ether beta-cyclodextrin binary and ternary complexes, Chem Pharm Bull (Tokyo), 51, 914, 10.1248/cpb.51.914
Ribeiro, 2003, Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with beta-cyclodextrin and its sulfobutyl ether derivative in solution and solid state, Eur J Pharm Sci, 20, 253, 10.1016/S0928-0987(03)00199-4
Rigler, 1986, Visualization by freeze fracture, in vitro and in vivo, of the products of fat digestion, J Lipid Res, 27, 836, 10.1016/S0022-2275(20)38788-5
Rodríguez-Spong, 2004, General principles of pharmaceutical solid polymorphism: a supramolecular perspective, Adv Drug Deliv Rev, 56, 241, 10.1016/j.addr.2003.10.005
Rohrs, 1999, Tablet dissolution affected by a moisture mediated solid-state interaction between drug and disintegrant, Pharm Res, 16, 1850, 10.1023/A:1018951309506
Roos, 1997, Frozen state transitions in relation to freeze drying, J Therm Anal Calorim, 48, 535, 10.1007/BF01979500
Ross, 1996, Thermodynamics of hydrogen bond and hydrophobic interactions in cyclodextrin complexes, Biophys J, 71, 2144, 10.1016/S0006-3495(96)79415-8
Rowe RC Sheskey PJ Quinn ME eds (2009) Handbook of Pharmaceutical Excipients, Pharmaceutical Press, London.
Rowinsky, 1991, Cardiac disturbances during the administration of taxol, J Clin Oncol, 9, 1704, 10.1200/JCO.1991.9.9.1704
Royall, 1998, Characterisation of the glass transition of an amorphous drug using modulated DSC, Pharm Res, 15, 1117, 10.1023/A:1011902816175
Rubin, 1966, Electron microscopic studies of triglyceride absorption in man, Gastroenterology, 50, 65, 10.1016/S0016-5085(66)80102-6
Rubino, 1987, The effects of cosolvents on the action of pharmaceutical buffers, J Parenter Sci Technol, 41, 45
Rubino JT (2002) Cosolvents and cosolvency, in Encylopedia of Pharmaceutical Technology (Swarbrick J and Boylan JC, eds) Marcel Dekker, New York.
Rubino, 1991, Influence of solute structure on deviations from the log-linear solubility equation in propylene glycol:water mixtures, J Pharm Sci, 80, 479, 10.1002/jps.2600800516
Rubino, 1990, Influence of solvent composition on the solubilities and solid-state properties of the sodium-salts of some drugs, Int J Pharm, 65, 141, 10.1016/0378-5173(90)90020-5
Rubino, 1987, Cosolvency and deviations from log-linear solubilization, Pharm Res, 4, 231, 10.1023/A:1016408211963
Ruble, 2006, The effect of commonly used vehicles on canine hematology and clinical chemistry values, J Am Assoc Lab Anim Sci, 45, 25
Rumondor, 2009, Evaluation of drug-polymer miscibility in amorphous solid dispersion systems, Pharm Res, 26, 2523, 10.1007/s11095-009-9970-7
Rumondor, 2009, Effects of polymer type and storage relative humidity on the kinetics of felodipine crystallization from amorphous solid dispersions, Pharm Res, 26, 2599, 10.1007/s11095-009-9974-3
Rumondor, 2010, Effect of polymer hygroscopicity on the phase behavior of amorphous solid dispersions in the presence of moisture, Mol Pharm, 7, 477, 10.1021/mp9002283
Sachs-Barrable, 2007, Lipid excipients Peceol and Gelucire 44/14 decrease P-glycoprotein mediated efflux of rhodamine 123 partially due to modifying P-glycoprotein protein expression within Caco-2 cells, J Pharm Pharm Sci, 10, 319
Saers, 1992, An investigation into the mechanisms of dissolution of alkyl p-aminobenzoates from polyethylene-glycol solid dispersions, Int J Pharm, 83, 211, 10.1016/0378-5173(82)90024-2
Saers, 1993, Physicochemical aspects of drug release. 16. The effect of storage on drug dissolution from solid dispersions and the influence of cooling rate and incorporation of surfactant, Int J Pharm, 90, 105, 10.1016/0378-5173(93)90147-8
Sahoo, 2011, Preparation and characterization of quercetin nanocrystals, J Pharm Sci, 100, 2379, 10.1002/jps.22446
Samaha, 1987, Solubilization of carbamazepin by different classes of nonionic surfactants and a bile-salt, Drug Dev Ind Pharm, 13, 93, 10.3109/03639048709040158
Sancin, 1999, Effects of ultrasound-assisted compaction on Ketoprofen/Eudragit S100 mixtures, Eur J Pharm Sci, 7, 207, 10.1016/S0928-0987(98)00022-0
Sarkar, 2010, Micellization of alkyl-propoxy-ethoxylate surfactants in water-polar organic solvent mixtures, Langmuir, 26, 10532, 10.1021/la100544w
Sassene, 2010, Precipitation of a poorly soluble model drug during in vitro lipolysis: characterization and dissolution of the precipitate, J Pharm Sci, 99, 4982, 10.1002/jps.22226
Sathigari, 2011, Single-step preparation and deagglomeration of itraconazole microflakes by supercritical antisolvent method for dissolution enhancement, J Pharm Sci, 100, 2952, 10.1002/jps.22524
Save, 1992, Studies on solid dispersions of nifedipine, Drug Dev Ind Pharm, 18, 1663, 10.3109/03639049209040893
Savolainen, 1998, Improved dissolution and bioavailability of phenytoin by sulfobutylether-beta-cyclodextrin ((SBE)(7m)-beta-CD) and hydroxypropyl-beta-cyclodextrin (HP-beta-CD) complexation, Int J Pharm, 165, 69, 10.1016/S0378-5173(98)00004-0
Schick JM (1966) Nonionic Surfactants, Marcel Dekker, New York.
Schott, 1973, Effect of chain length in homologous series of anionic surfactants on irritant action and toxicity, J Pharm Sci, 62, 341, 10.1002/jps.2600620242
Schott, 1975, Effect of inorganic additives on solutions of nonionic surfactants II, J Pharm Sci, 64, 658, 10.1002/jps.2600640419
Schou, 1958, Lithium studies. 1. Toxicity, Acta Pharmacol Toxicol (Copenh), 15, 70, 10.1111/j.1600-0773.1958.tb00287.x
Schrijvers, 1993, Coping with toxicities of docetaxel (Taxotere), Ann Oncol, 4, 610, 10.1093/oxfordjournals.annonc.a058599
Schultheiss, 2009, Pharmaceutical cocrystals and their physicochemical properties, Cryst Growth Des, 9, 2950, 10.1021/cg900129f
Schulze, 2005, Excipient effects on gastrointestinal transit and drug absorption in beagle dogs, Int J Pharm, 300, 67, 10.1016/j.ijpharm.2005.05.004
Schuurhuis, 1990, The polyoxyethylene castor oil Cremophor EL modifies multidrug resistance, Br J Cancer, 62, 591, 10.1038/bjc.1990.335
Seeballuck, 2004, Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model, Pharm Res, 21, 2320, 10.1007/s11095-004-7684-4
Seedher, 2009, Co-solvent solubilization of some poorly-soluble antidiabetic drugs, Pharm Dev Technol, 14, 185, 10.1080/10837450802498894
Seefeldt, 2007, Crystallization pathways and kinetics of carbamazepine-nicotinamide cocrystals from the amorphous state by in situ thermomicroscopy, spectroscopy, and calorimetry studies, J Pharm Sci, 96, 1147, 10.1002/jps.20945
Sek, 2006, Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone, J Pharm Pharmacol, 58, 809, 10.1211/jpp.58.6.0011
Sek, 2002, Evaluation of the in-vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products, J Pharm Pharmacol, 54, 29, 10.1211/0022357021771896
Sekine, 1985, Improvement of bioavailability of poorly absorbed drugs. II. Effect of medium chain glyceride base on the intestinal absorption of cefmetazole sodium in rats and dogs, J Pharmacobiodyn, 8, 286, 10.1248/bpb1978.8.286
Seo, 2003, The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer, Int J Pharm, 259, 161, 10.1016/S0378-5173(03)00228-X
Serajuddin, 1985, Effect of diffusion layer pH and solubility on the dissolution rate of pharmaceutical acids and their sodium salts. II. Salicylic acid, theophylline, and benzoic acid, J Pharm Sci, 74, 148, 10.1002/jps.2600740209
Serajuddin, 1985, Effect of diffusion layer pH and solubility on the dissolution rate of pharmaceutical bases and their hydrochloride salts. I. Phenazopyridine, J Pharm Sci, 74, 142, 10.1002/jps.2600740208
Serajuddin ATM Pudipeddi M (2002) Salt-selection strategies, in Handbook of Pharmaceutical Salts: Properties, Selection and Use ( Stahl PH Wermuth GH , eds) pp 135–160, Wiley-VCH, Weinheim.
Serajuddin, 1987, Common ion effect on solubility and dissolution rate of the sodium salt of an organic acid, J Pharm Pharmacol, 39, 587, 10.1111/j.2042-7158.1987.tb03434.x
Serajuddin, 1990, Improved dissolution of a poorly water-soluble drug from solid dispersions in polyethylene glycol: polysorbate 80 mixtures, J Pharm Sci, 79, 463, 10.1002/jps.2600790524
Serajuddin, 1986, Preformulation study of a poorly water-soluble drug, alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol: selection of the base for dosage form design, J Pharm Sci, 75, 492, 10.1002/jps.2600750514
Serajuddin, 1988, Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions, J Pharm Sci, 77, 414, 10.1002/jps.2600770512
Serratoni, 2007, Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system, Eur J Pharm Biopharm, 65, 94, 10.1016/j.ejpb.2006.07.011
Sethia, 2002, Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method, J Pharm Sci, 91, 1948, 10.1002/jps.10186
Sethia, 2004, Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods, Int J Pharm, 272, 1, 10.1016/j.ijpharm.2003.11.025
Sha X Yan G Wu Y Li J Fang X (2005) Effect of self-microemulsifying drug delivery systems containing Labrasol on tight junctions in Caco-2 cells. Eur J Pharm Sci 24:477–486.
Shah, 2011, Recent advances and novel strategies in pre-clinical formulation development: an overview, J Control Release, 156, 281, 10.1016/j.jconrel.2011.07.003
Shah, 2012, Development of solid self-emulsifying drug delivery system (SEDDS) I: Use of poloxamer 188 as both solidifying and emulsifying agent for lipids, Pharm Res, 29, 2817, 10.1007/s11095-012-0704-x
Shah, 1995, Preformulation study of etoposide. 2. Increased solubility and dissolution rate by solid-solid dispersions, Int J Pharm, 113, 103, 10.1016/0378-5173(94)00195-B
Shah, 2001, Cubic phase gels as drug delivery systems, Adv Drug Deliv Rev, 47, 229, 10.1016/S0169-409X(01)00108-9
Shalel, 2002, The mechanism of hemolysis by surfactants: effect of solution composition, J Colloid Interface Sci, 252, 66, 10.1006/jcis.2002.8474
Shamblin, 2000, Interpretation of relaxation time constants for amorphous pharmaceutical systems, J Pharm Sci, 89, 417, 10.1002/(SICI)1520-6017(200003)89:3<417::AID-JPS12>3.0.CO;2-V
Shamblin, 1999, Characterization of the time scales of molecular motion in pharmaceutically important glasses, J Phys Chem B, 103, 4113, 10.1021/jp983964+
Shan, 2008, The role of cocrystals in pharmaceutical science, Drug Discov Today, 13, 440, 10.1016/j.drudis.2008.03.004
Shanker, 1994, Selection of appropriate salt form(s) for new drug candidates, Pharm Res, 11, s-236
Sharma, 2011, Evaluation of a crystalline nanosuspension: polymorphism, process induced transformation and in vivo studies, Int J Pharm, 408, 138, 10.1016/j.ijpharm.2011.01.032
Shayeganpour, 2008, The impact of experimental hyperlipidemia on the distribution and metabolism of amiodarone in rat, Int J Pharm, 361, 78, 10.1016/j.ijpharm.2008.05.019
Sheen, 1995, Formulation studies of a poorly water-soluble drug in solid dispersions to improve bioavailability, Int J Pharm, 118, 221, 10.1016/0378-5173(94)00366-D
Shen, 2008, Modulating effect of polyethylene glycol on the intestinal transport and absorption of prednisolone, methylprednisolone and quinidine in rats by in-vitro and in-situ absorption studies, J Pharm Pharmacol, 60, 1633, 10.1211/jpp.60.12.0009
Shen, 1992, Miscibility and phase-separation in poly(methyl methacrylate) poly(vinyl chloride) blends: study of thermodynamics by thermal-analysis, Macromolecules, 25, 721, 10.1021/ma00028a034
Sheng, 2006, Solubilization and dissolution of insoluble weak acid, ketoprofen: effects of pH combined with surfactant, Eur J Pharm Sci, 29, 306, 10.1016/j.ejps.2006.06.006
Shi, 2005, Current advances in sustained-release systems for parenteral drug delivery, Expert Opin Drug Deliv, 2, 1039, 10.1517/17425247.2.6.1039
Shi, 2009, Recent advances in intravenous delivery of poorly water-soluble compounds, Expert Opin Drug Deliv, 6, 1261, 10.1517/17425240903307423
Shiau, 1981, Mechanisms of intestinal fat absorption, Am J Physiol, 240, G1
Shiau, 1985, Mechanisms maintaining a low-pH microclimate in the intestine, Am J Physiol, 248, G608
Shimpi, 2005, Stabilization and improved in vivo performance of amorphous etoricoxib using Gelucire 50/13, Pharm Res, 22, 1727, 10.1007/s11095-005-6694-1
Shin, 2003, Physicochemical characterization of solid dispersion of furosemide with TPGS, Int J Pharm, 251, 79, 10.1016/S0378-5173(02)00586-0
Shinde, 2008, Enhanced solubility and dissolution rate of lamotrigine by inclusion complexation and solid dispersion technique, J Pharm Pharmacol, 60, 1121, 10.1211/jpp.60.9.0002
Shinozaki, 2006, Micronization and polymorphic conversion of tolbutamide and barbital by rapid expansion of supercritical solutions, Drug Dev Ind Pharm, 32, 877, 10.1080/03639040500529994
Shiraki, 2008, Dissolution improvement and the mechanism of the improvement from cocrystallization of poorly water-soluble compounds, Pharm Res, 25, 2581, 10.1007/s11095-008-9676-2
Shono, 2011, Precipitation in the small intestine may play a more important role in the in vivo performance of poorly soluble weak bases in the fasted state: case example nelfinavir, Eur J Pharm Biopharm, 79, 349, 10.1016/j.ejpb.2011.04.005
Sigfridsson, 2011, Usefulness of a nanoparticle formulation to investigate some hemodynamic parameters of a poorly soluble compound, J Pharm Sci, 100, 2194, 10.1002/jps.22440
Sigfridsson, 2007, A formulation comparison, using a solution and different nanosuspensions of a poorly soluble compound, Eur J Pharm Biopharm, 67, 540, 10.1016/j.ejpb.2007.02.008
Sigfridsson, 2011, A formulation comparison between micro- and nanosuspensions: the importance of particle size for absorption of a model compound, following repeated oral administration to rats during early development, Drug Dev Ind Pharm, 37, 185, 10.3109/03639045.2010.504209
Simha, 1962, On a general relation involving the glass temperature and coefficients of expansion of polymers, J Chem Phys, 37, 1003, 10.1063/1.1733201
Simonelli, 1976, Dissolution rates of high energy sulfathiazole-povidone coprecipitates. II. Characterization of form of drug controlling its dissolution rate via solubility studies, J Pharm Sci, 65, 355, 10.1002/jps.2600650310
Singhal, 2004, Drug polymorphism and dosage form design: a practical perspective, Adv Drug Deliv Rev, 56, 335, 10.1016/j.addr.2003.10.008
Sinha, 2009, Solid dispersion: an alternative technique for bioavailability enhancement of poorly soluble drugs, J Dispersion Sci Technol, 30, 1458, 10.1080/01932690903120136
Sinko PJ (2006) Martin’s Physical Pharmacy and Pharmaceutical Sciences, Lippincott Williams and Wilkins, Philadelphia.
Sipahi, 1989, Contribution of plasma protein and lipoproteins to intestinal lymph: comparison of long-chain with medium-chain triglyceride duodenal infusion, Lymphology, 22, 13
Sirois P (2007) Feasibility assessment and considerations for scaling initial prototype lipid-based formulations to phase I/II clinical trial batches, in Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water Soluble Drugs ( Hauss DJ ed) pp 63–78, Informa Healthcare, Inc., New York.
Six, 2003, Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, Part II, Pharm Res, 20, 1047, 10.1023/A:1024414423779
Six, 2003, Identification of phase separation in solid dispersions of itraconazole and Eudragit E100 using microthermal analysis, Pharm Res, 20, 135, 10.1023/A:1022219429708
Six, 2001, Investigation of thermal properties of glassy itraconazole: identification of a monotropic mesophase, Thermochim Acta, 376, 175, 10.1016/S0040-6031(01)00563-9
Six, 2004, Increased physical stability and improved dissolution properties of itraconazole, a class II drug, by solid dispersions that combine fast- and slow-dissolving polymers, J Pharm Sci, 93, 124, 10.1002/jps.10522
Sjostrom, 1992, Preparation of submicron drug particles in lecithin-stabilized O/W emulsions. 1. Model studies of the precipitation cholesteryl acetate, Int J Pharm, 88, 53, 10.1016/0378-5173(92)90303-J
Smith, 2011, Cocrystals of quercetin with improved solubility and oral bioavailability, Mol Pharm, 8, 1867, 10.1021/mp200209j
Smith, 2005, Effect of SBE7-beta-cyclodextrin complexation on carbamazepine release from sustained release beads, Eur J Pharm Biopharm, 60, 73, 10.1016/j.ejpb.2004.12.001
Snodin, 2006, Residues of genotoxic alkyl mesylates in mesylate salt drug substances: real or imaginary problems?, Regul Toxicol Pharmacol, 45, 79, 10.1016/j.yrtph.2006.02.003
Söderlind, 2003, The usefulness of sugar surfactants as solubilizing agents in parenteral formulations, Int J Pharm, 252, 61, 10.1016/S0378-5173(02)00599-9
Sollohub, 2010, Spray drying technique. II. Current applications in pharmaceutical technology, J Pharm Sci, 99, 587, 10.1002/jps.21963
Sotthivirat, 2007, Controlled porosity-osmotic pump pellets of a poorly water-soluble drug using sulfobutylether-beta-cyclodextrin, (SBE) 7M-beta-CD, as a solubilizing and osmotic agent, J Pharm Sci, 96, 2364, 10.1002/jps.20891
Southard, 1992, Dissolution of ionizable drugs into unbuffered solution: a comprehensive model for mass transport and reaction in the rotating disk geometry, Pharm Res, 9, 58, 10.1023/A:1018979727118
Sparreboom, 1999, Cremophor EL-mediated alteration of paclitaxel distribution in human blood: clinical pharmacokinetic implications, Cancer Res, 59, 1454
Stahl PH (2003) Preparation of water-soluble compounds through salt formation, in The Practice of Medicinal Chemistry, 2nd Edition ( Wermuth CG ed) pp 601–615, London, Elsevier.
Stahl PH Wermuth GH (2002) Handbook of Pharmaceutical Salts: Properties, Selection and Use, Wiley-VCH, Weinheim.
Stanton, 2008, Physicochemical properties of pharmaceutical co-crystals: A case study of ten AMG 517 co-crystals, Cryst Growth Des, 8, 3856, 10.1021/cg800173d
Stanton, 2010, Improved pharmacokinetics of AMG 517 through co-crystallization. Part 1: comparison of two acids with corresponding amide co-crystals, J Pharm Sci, 99, 3769, 10.1002/jps.22181
Stanton, 2011, Improved pharmacokinetics of AMG 517 through co-crystallization. Part 2. Analysis of 12 carboxylic acid co-crystals, J Pharm Sci, 100, 2734, 10.1002/jps.22502
Stanton, 2009, Drug substance and former structure property relationships in 15 diverse pharmaceutical co-crystals, Cryst Growth Des, 9, 1344, 10.1021/cg8005019
Stevens, 2010, Salt or co-crystal? Determination of protonation state by X-ray photoelectron spectroscopy (XPS), J Pharm Sci, 99, 4453, 10.1002/jps.22164
Streng, 1984, General treatment of pH-solubility profiles of weak acids and bases and the effects of different acids on the solubility of a weak base, J Pharm Sci, 73, 1679, 10.1002/jps.2600731203
Strickley RG (2007) Currently marketed oral lipid-based dosage forms: enhancing the bioavailability of poorly water soluble drugs, in Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water Soluble Drugs ( Hauss DJ ed) pp 1–31, Informa Healthcare, Inc., New York.
Strickley RG Oliyai R (2007) Solubilizing vehicles for oral formulation development, in Solvent Systems and Their Selection in Pharmaceutics and Biopharmaceutics ( Augustijns P Brewster M eds) pp 257–308, Springer, New York.
Su, 2009, Micronization of nabumetone using the rapid expansion of supercritical solution (RESS) process, J Supercrit Fluids, 50, 69, 10.1016/j.supflu.2009.04.013
Sugano, 2008, Theoretical comparison of hydrodynamic diffusion layer models used for dissolution simulation in drug discovery and development, Int J Pharm, 363, 73, 10.1016/j.ijpharm.2008.07.002
Suhonen, 1995, Ocular absorption and irritation of pilocarpine prodrug is modified with buffer, polymer, and cyclodextrin in the eyedrop, Pharm Res, 12, 529, 10.1023/A:1016297728396
Summers, 1976, Preparation and properties of solid dispersion system containing citric acid and primidone, J Pharm Sci, 65, 1613, 10.1002/jps.2600651113
Sun, 2011, Nanonization of itraconazole by high pressure homogenization: stabilizer optimization and effect of particle size on oral absorption, J Pharm Sci, 100, 3365, 10.1002/jps.22587
Sun, 2010, Solubilities of crystalline drugs in polymers: an improved analytical method and comparison of solubilities of indomethacin and nifedipine in PVP, PVP/VA, and PVAc, J Pharm Sci, 99, 4023, 10.1002/jps.22251
Sunesen VH Vedelsdal R Kristensen HG Christrup L Mullertz A (2005) Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug. Eur J Pharmaceutical Sci 24:297–303.
Suresh, 2007, Preparation, characterization, and in vitro and in vivo evaluation of lovastatin solid lipid nanoparticles, AAPS PharmSciTech, 8, E162, 10.1208/pt0801024
Suzuki, 1998, Influence of water-soluble polymers on the dissolution of nifedipine solid dispersions with combined carriers, Chem Pharm Bull (Tokyo), 46, 482, 10.1248/cpb.46.482
Szatmari I Vargay Z (1988) Pharmacokinetics of dimethyl-beta-cyclodextrin in rats, in Proceedings of the 4th International Symposium on Cyclodextrins (Duchene D, ed) pp 407–413; 1988 April 20–22; Munich, Germany; Kluwer Academic Publishers, Norwell, MA.
Szejtli, 1994, Medicinal applications of cyclodextrins, Med Res Rev, 14, 353, 10.1002/med.2610140304
Taillardat A Diederich A Sutter B Kalb O Cuiné JF (2007) Use of in vitro dispersion and digestion tests to explain the in vivo performance of two lipid- based oral drug delivery systems in man. Am Pharm Rev 10:40–46.
Tajarobi, 2011, The influence of crystallization inhibition of HPMC and HPMCAS on model substance dissolution and release in swellable matrix tablets, Eur J Pharm Biopharm, 78, 125, 10.1016/j.ejpb.2010.11.020
Takeuchi, 2005, Solid dispersion particles of amorphous indomethacin with fine porous silica particles by using spray-drying method, Int J Pharm, 293, 155, 10.1016/j.ijpharm.2004.12.019
Takisawa, 1993, Interactions of amphiphilic drugs with alpha-cyclodextrin, beta-cyclodextrin, and gamma-cyclodextrin, Colloid Polym Sci, 271, 499, 10.1007/BF00657395
Tan, 2012, Hybrid nanomaterials that mimic the food effect: controlling enzymatic digestion for enhanced oral drug absorption, Angew Chem Int Ed Engl, 51, 5475, 10.1002/anie.201200409
Tan, 2009, Silica-lipid hybrid (SLH) microcapsules: a novel oral delivery system for poorly soluble drugs, J Control Release, 134, 62, 10.1016/j.jconrel.2008.10.014
Tan, 1991, Studies on complexation between beta-cyclodextrin and bile-salts, Int J Pharm, 74, 127, 10.1016/0378-5173(91)90229-H
Tanford C (1980) The Hydrophobic Rffect: Formation of Micelles and Biological Membranes, Wiley, New York.
Tang, 2008, Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms, Drug Discov Today, 13, 606, 10.1016/j.drudis.2008.04.006
Taniguchi T Yamamoto K Kobayashi T (1998) Precipitate formed by thiopentone and vecuronium causes pulmonary embolism. Can J Anaesth 45:347–351.
Tanno, 2004, Evaluation of hypromellose acetate succinate (HPMCAS) as a carrier in solid dispersions, Drug Dev Ind Pharm, 30, 9, 10.1081/DDC-120027506
Tantishaiyakul, 1999, Properties of solid dispersions of piroxicam in polyvinylpyrrolidone, Int J Pharm, 181, 143, 10.1016/S0378-5173(99)00070-8
Tao, 2009, Preparation and evaluation of itraconazole dihydrochloride for the solubility and dissolution rate enhancement, Int J Pharm, 367, 109, 10.1016/j.ijpharm.2008.09.034
Tarsa, 2010, The influence of aqueous content in small scale salt screening: improving hit rate for weakly basic, low solubility drugs, Eur J Pharm Sci, 41, 23, 10.1016/j.ejps.2010.05.009
Tavares LC (2007) Breakage of single particles: quasi-static, in Handbook of Powder Technology ( Williams JC Allen T eds) pp 3–68, Elsevier, New York.
Taylor, 1997, Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions, Pharm Res, 14, 1691, 10.1023/A:1012167410376
Teasdale, 2009, Mechanism and processing parameters affecting the formation of methyl methanesulfonate from methanol and methanesulfonic acid: an illustrative example for sulfonate ester impurity formation, Org Process Res Dev, 13, 429, 10.1021/op800192a
Thakur, 2006, Formation of phenytoin nanoparticles using rapid expansion of supercritical solution with solid cosolvent (RESS-SC) process, Int J Pharm, 308, 190, 10.1016/j.ijpharm.2005.11.005
Thayyil, 2008, Is the Johari-Goldstein beta-relaxation universal?, Philos Mag, 88, 4007, 10.1080/14786430802270082
The Merck Index (2006) 14th ed. Merck & Co. Inc., Whitehouse Station, NJ.
Thies, 2003, A supercritical fluid-based coating technology. 1. Process considerations, J Microencapsul, 20, 87, 10.3109/02652040309178051
Thomas, 1996, Solubility, melting point and salting-out relationships in a group of secondary amine hydrochloride salts, Int J Pharm, 130, 179, 10.1016/0378-5173(95)04269-5
Thomas, 2012, In vitro and in vivo performance of novel supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS), J Control Release, 160, 25, 10.1016/j.jconrel.2012.02.027
Thombre, 2011, Improved ziprasidone formulations with enhanced bioavailability in the fasted state and a reduced food effect, Pharm Res, 28, 3159, 10.1007/s11095-011-0505-7
Thombre, 2012, In vitro and in vivo characterization of amorphous, nanocrystalline, and crystalline ziprasidone formulations, Int J Pharm, 428, 8, 10.1016/j.ijpharm.2012.02.004
Thompson, 1997, Cyclodextrins: enabling excipients: their present and future use in pharmaceuticals, Crit Rev Ther Drug Carrier Syst, 14, 1, 10.1615/CritRevTherDrugCarrierSyst.v14.i1.10
Tokumura, 1986, Enhancement of bioavailability of cinnarizine from its beta-cyclodextrin complex on oral administration with DL-phenylalanine as a competing agent, J Pharm Sci, 75, 391, 10.1002/jps.2600750415
Tombari, 2008, Calorimetric relaxation in pharmaceutical molecular glasses and its utility in understanding their stability against crystallization, J Phys Chem B, 112, 10806, 10.1021/jp801794a
Tombari, 2008, Vibrational and configurational specific heats during isothermal structural relaxation of a glass to equilibrium liquid, Phys Rev B, 78, 144203-1, 10.1103/PhysRevB.78.144203
Tomita, 1992, Differences in the enhancing effects of sodium caprate on colonic and jejunal drug absorption, Pharm Res, 9, 648, 10.1023/A:1015854127486
Tommasini, 2004, Combined effect of pH and polysorbates with cyclodextrins on solubilization of naringenin, J Pharm Biomed Anal, 36, 327, 10.1016/j.jpba.2004.06.013
Tomsic, 2006, Ternary systems of nonionic surfactant Brij 35, water and various simple alcohols: structural investigations by small-angle X-ray scattering and dynamic light scattering, J Colloid Interface Sci, 294, 194, 10.1016/j.jcis.2005.06.088
Tong, 1999, Solid-state characteristics of amorphous sodium indomethacin relative to its free acid, Pharm Res, 16, 1186, 10.1023/A:1018985110956
Tong, 2001, A study of amorphous molecular dispersions of indomethacin and its sodium salt, J Pharm Sci, 90, 1991, 10.1002/jps.1150
Tong, 1991, Structural effects on the binding of amine drugs with the diphenylmethyl functionality to cyclodextrins. I. A microcalorimetric study, Pharm Res, 8, 951, 10.1023/A:1015880218535
Tong, 1998, In situ salt screening: a useful technique for discovery support and preformulation studies, Pharm Dev Technol, 3, 215, 10.3109/10837459809028498
Tønsberg, 2011, Effect of bile on the oral absorption of halofantrine in polyethylene glycol 400 and polysorbate 80 formulations dosed to bile duct cannulated rats, J Pharm Pharmacol, 63, 817, 10.1111/j.2042-7158.2011.01286.x
Torosian, 1973, Hazards of bromides in proprietary medication, Am J Hosp Pharm, 30, 716
Towler, 2008, An investigation into the influence of counterion on the properties of some amorphous organic salts, Mol Pharm, 5, 946, 10.1021/mp8000342
Tozuka, 2006, Ibuprofen-cyclodextrin inclusion complex formation using supercritical carbon dioxide, J Incl Phenom Macrocycl Chem, 56, 33, 10.1007/s10847-006-9057-6
Trägner, 1987, Biphasic interaction of Triton detergents with the erythrocyte membrane, Biochem J, 244, 605, 10.1042/bj2440605
Trask, 2004, Solvent-drop grinding: green polymorph control of cocrystallisation, Chem Commun (Camb), 7:, 890, 10.1039/b400978a
Treiner, 1994, The thermodynamics of micellar solubilization of neutral solutes in aqueous binary surfactant systems, Chem Soc Rev, 23, 349, 10.1039/cs9942300349
Tso, 1995, Intestinal digestion, absorption, and transport of structured triglycerides and cholesterol in rats, Am J Physiol, 268, G568
Tsui, 2010, Study of heat of micellization and phase separation for Pluronic aqueous solutions by using a high sensitivity differential scanning calorimetry, Colloid Polym Sci, 288, 1687, 10.1007/s00396-010-2308-5
Turk, 2010, Formation of submicron poorly water-soluble drugs by rapid expansion of supercritical solution (RESS): results for naproxen, J Supercrit Fluids, 55, 778, 10.1016/j.supflu.2010.09.023
Turk, 2002, Micronization of pharmaceutical substances by the rapid expansion of supercritical solutions (RESS): a promising method to improve bioavailability of poorly soluble pharmaceutical agents, J Supercrit Fluids, 22, 75, 10.1016/S0896-8446(01)00109-7
Tytgat, 1971, Synthesis and transport of lipoprotein particles by intestinal absorptive cells in man, J Clin Invest, 50, 2065, 10.1172/JCI106700
Uekama, 2002, Recent aspects of pharmaceutical application of cyclodextrins, J Incl Phenom Macrocycl Chem, 44, 3, 10.1023/A:1023007032444
Uekama, 2004, Design and evaluation of cyclodextrin-based drug formulation, Chem Pharm Bull (Tokyo), 52, 900, 10.1248/cpb.52.900
Uekama, 1982, Inclusion complexations of steroid-hormones with cyclodextrins in water and in solid-phase, Int J Pharm, 10, 1, 10.1016/0378-5173(82)90057-6
Uekama, 1990, Design and in vitro evaluation of slow-release dosage form of piretanide: utility of beta-cyclodextrin:cellulose derivative combination as a modified-release drug carrier, J Pharm Sci, 79, 244, 10.1002/jps.2600790314
Uekama, 1983, Improvement of dissolution and absorption characteristics of benzodiazepines by cyclodextrin complexation, Int J Pharm, 16, 327, 10.1016/0378-5173(83)90151-5
Unowsky, 1988, Effect of medium chain glycerides on enteral and rectal absorption of beta-lactam and aminoglycoside antibiotics, Chemotherapy, 34, 272, 10.1159/000238580
Usui, 1997, Inhibitory effects of water-soluble polymers on precipitation of RS-8359, Int J Pharm, 154, 59, 10.1016/S0378-5173(97)00129-4
Vaddi HK Khan MA Reddy IK (2007) Ocular, nasal and otic drug delivery, in Gibaldi’s Drug Delivery Systems in Pharmaceutical Care ( Gibaldi M Desai A Lee M eds) pp 59–78, Bethesda, MD, American Society of Health-System Pharmacists.
Valero, 2003, Effect of PVP K-25 on the formation of the naproxen:beta-ciclodextrin complex, Int J Pharm, 253, 97, 10.1016/S0378-5173(02)00664-6
Valizadeh, 2004, Physicochemical characterization of solid dispersions of indomethacin with PEG 6000, Myrj 52, lactose, sorbitol, dextrin, and Eudragit E100, Drug Dev Ind Pharm, 30, 303, 10.1081/DDC-120030426
van den Bosch, 1965, On the positional specificity of phospholipase A from pancreas, Biochim Biophys Acta, 98, 657, 10.1016/0005-2760(65)90168-2
Van den Mooter, 1998, Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30, Int J Pharm, 164, 67, 10.1016/S0378-5173(97)00401-8
Vandecruys, 2007, Use of a screening method to determine excipients which optimize the extent and stability of supersaturated drug solutions and application of this system to solid formulation design, Int J Pharm, 342, 168, 10.1016/j.ijpharm.2007.05.006
Van den Mooter, 2001, Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25, Eur J Pharm Sci, 12, 261, 10.1016/S0928-0987(00)00173-1
Van Drooge, 2004, Incorporation of lipophilic drugs in sugar glasses by lyophilization using a mixture of water and tertiary butyl alcohol as solvent, J Pharm Sci, 93, 713, 10.1002/jps.10590
van Drooge, 2006, Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques, Int J Pharm, 310, 220, 10.1016/j.ijpharm.2005.12.007
Van Eerdenbrugh, 2011, Influence of particle size on the ultraviolet spectrum of particulate-containing solutions: implications for in-situ concentration monitoring using UV/Vis fiber-optic probes, Pharm Res, 28, 1643, 10.1007/s11095-011-0399-4
Van Eerdenbrugh, 2010, Crystallization tendency of active pharmaceutical ingredients following rapid solvent evaporation: classification and comparison with crystallization tendency from undercooled melts, J Pharm Sci, 99, 3826, 10.1002/jps.22214
Van Eerdenbrugh, 2008, Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products, Int J Pharm, 364, 64, 10.1016/j.ijpharm.2008.07.023
Van Eerdenbrugh, 2009, Itraconazole/TPGS/Aerosil200 solid dispersions: characterization, physical stability and in vivo performance, Eur J Pharm Sci, 38, 270, 10.1016/j.ejps.2009.08.002
Van Eerdenbrugh, 2010, Solubility increases associated with crystalline drug nanoparticles: methodologies and significance, Mol Pharm, 7, 1858, 10.1021/mp100209b
Van Hees, 1999, Application of supercritical carbon dioxide for the preparation of a piroxicam-beta-cyclodextrin inclusion compound, Pharm Res, 16, 1864, 10.1023/A:1018955410414
Van Speybroeck, 2009, Ordered mesoporous silica material SBA-15: a broad-spectrum formulation platform for poorly soluble drugs, J Pharm Sci, 98, 2648, 10.1002/jps.21638
Van Speybroeck, 2010, Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica, Eur J Pharm Sci, 41, 623, 10.1016/j.ejps.2010.09.002
van Speybroeck, 2011, Preventing release in the acidic environment of the stomach via occlusion in ordered mesoporous silica enhances the absorption of poorly soluble weakly acidic drugs, J Pharm Sci, 100, 4864, 10.1002/jps.22703
Van Speybroeck, 2010, Combined use of ordered mesoporous silica and precipitation inhibitors for improved oral absorption of the poorly soluble weak base itraconazole, Eur J Pharm Biopharm, 75, 354, 10.1016/j.ejpb.2010.04.009
Van Speybroeck, 2012, Incomplete desorption of liquid excipients reduces the in vitro and in vivo performance of self-emulsifying drug delivery systems solidified by adsorption onto an inorganic mesoporous carrier, Mol Pharm, 9:, 2750, 10.1021/mp300298z
van Stam, 1996, 2-Naphthol complexation by beta-cyclodextrin: influence of added short linear alcohols, J Phys Chem, 100, 19959, 10.1021/jp961575e
Variankaval, 2006, Preparation and solid-state characterization of nonstoichiometric cocrystals off a phosphodiesterase-IV inhibitor and L-tartaric acid, Cryst Growth Des, 6, 690, 10.1021/cg050462u
Varma, 2005, Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo, Eur J Pharmaceutical Sci, 25, 445, 10.1016/j.ejps.2005.04.003
Vasanthavada M Serajuddin ATM (2007) Lipid-based self-emulsifying solid dispersions, in Oral Lipid-Based Formulations: Enhancing the Bioavailability of Poorly Water-Soluble Drugs ( Hauss DJ ed) pp 149–184, Informa Healthcare, New York.
Vasanthavada, 2004, Phase behavior of amorphous molecular dispersions. I. Determination of the degree and mechanism of solid solubility, Pharm Res, 21, 1598, 10.1023/B:PHAM.0000041454.76342.0e
Vasanthavada, 2005, Phase behavior of amorphous molecular dispersions. II. Role of hydrogen bonding in solid solubility and phase separation kinetics, Pharm Res, 22, 440, 10.1007/s11095-004-1882-y
Veiga, 2001, Influence of the preparation method on the physicochemical properties of tolbutamide/cyclodextrin binary systems, Drug Dev Ind Pharm, 27, 523, 10.1081/DDC-100105177
Veiga, 1996, Inclusion complexation of tolbutamide with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin, Int J Pharm, 129, 63, 10.1016/0378-5173(95)04243-1
Veiga, 1998, Solubility study of tolbutamide in monocomponent and dicomponent solutions of water, Int J Pharm, 160, 43, 10.1016/S0378-5173(97)00295-0
Veiga, 1993, Dissolution behavior of drugs from binary and ternary-systems, Int J Pharm, 93, 215, 10.1016/0378-5173(93)90180-N
Verbeeck, 2006, Generic substitution: the use of medicinal products containing different salts and implications for safety and efficacy, Eur J Pharm Sci, 28, 1, 10.1016/j.ejps.2005.12.001
Verheyen, 2002, Mechanism of increased dissolution of diazepam and temazepam from polyethylene glycol 6000 solid dispersions, Int J Pharm, 249, 45, 10.1016/S0378-5173(02)00532-X
Verreck, 2003, Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion. Part I, Int J Pharm, 251, 165, 10.1016/S0378-5173(02)00591-4
Viernstein, 1992, Similar central actions of intravenous methohexitone suspension and solution in the rabbit, J Pharm Pharmacol, 44, 66, 10.1111/j.2042-7158.1992.tb14368.x
Vilhelmsen, 2005, Effect of a melt agglomeration process on agglomerates containing solid dispersions, Int J Pharm, 303, 132, 10.1016/j.ijpharm.2005.07.012
Villaverde, 2004, Preparation and characterization of inclusion complex of norflurazon and beta-cyclodextrin to improve herbicide formulations, J Agric Food Chem, 52, 864, 10.1021/jf0350358
Visalakshi, 2005, Behavior of moisture gain and equilibrium moisture contents (EMC) of various drug substances and correlation with compendial information on hygroscopicity and loss on drying, Pharm Dev Technol, 10, 489, 10.1080/10837450500299883
Viscomi, 2008, Crystal forms of rifaximin and their effect on pharmaceutical properties, CrystEngComm, 10, 1074, 10.1039/b717887e
Vogt, 2008, Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: comparison with commercial preparations, Eur J Pharm Biopharm, 68, 283, 10.1016/j.ejpb.2007.05.010
Volcheck, 1998, Anaphylaxis to intravenous cyclosporine and tolerance to oral cyclosporine: case report and review, Ann Allergy Asthma Immunol, 80, 159, 10.1016/S1081-1206(10)62949-3
Völgyi, 2010, Study of pH-dependent solubility of organic bases: revisit of Henderson-Hasselbalch relationship, Anal Chim Acta, 673, 40, 10.1016/j.aca.2010.05.022
Vyazovkin, 2005, Physical stability and relaxation of amorphous indomethacin, J Phys Chem B, 109, 18637, 10.1021/jp052985i
Walkling, 1983, Xilobam: effect of salt form on pharmaceutical properties, Drug Dev Ind Pharm, 9, 809, 10.3109/03639048309039889
Walsh, 2003, Crystal engineering of the composition of pharmaceutical phases, Chem Commun (Camb), 2, 186, 10.1039/b208574g
Walton, 1970, Anhydrotetracycline and 4-epianhydrotetracycline in market tetracyclines and aged tetracycline products, J Pharm Sci, 59, 1160, 10.1002/jps.2600590822
Wandel, 2003, “Inactive” excipients such as Cremophor can affect in vivo drug disposition, Clin Pharmacol Ther, 73, 394, 10.1016/S0009-9236(03)00010-9
Wang, 2006, Preparation and evaluation of solid dispersions of nitrendipine prepared with fine silica particles using the melt-mixing method, Chem Pharm Bull (Tokyo), 54, 37, 10.1248/cpb.54.37
Wang, 2011, Development and in vitro evaluation of deacety mycoepoxydiene nanosuspension, Colloids Surf B Biointerfaces, 83, 189, 10.1016/j.colsurfb.2010.10.029
Wang, 2010, In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery, Nanotechnology, 21, 155104, 10.1088/0957-4484/21/15/155104
Wang, 1980, Review of excipients and pH’s for parenteral products used in the United States, J Parenter Drug Assoc, 34, 452
Wang, 2011, Formulation and pharmacokinetic evaluation of a paclitaxel nanosuspension for intravenous delivery, Int J Nanomedicine, 6, 1497
Wang, 2010, Solid self-emulsifying nitrendipine pellets: preparation and in vitro/in vivo evaluation, Int J Pharm, 383, 1, 10.1016/j.ijpharm.2009.08.014
Wang, 2002, Solubility of E2050 at various pH: a case in which apparent solubility is affected by the amount of excess solid, J Pharm Sci, 91, 1445, 10.1002/jps.10107
Ward, 1993, Studies in phlebitis. IV. Injection rate and amiodarone-induced phlebitis, J Parenter Sci Technol, 47, 40
Ware, 2004, An automated approach to salt selection for new unique trazodone salts, Pharm Res, 21, 177, 10.1023/B:PHAM.0000012167.60180.c3
Warnakula, 2011, New insights into how the intestine can regulate lipid homeostasis and impact vascular disease: frontiers for new pharmaceutical therapies to lower cardiovascular disease risk, Can J Cardiol, 27, 183, 10.1016/j.cjca.2010.12.020
Warren, 2011, Real time evolution of liquid crystalline nanostructure during the digestion of formulation lipids using synchrotron small-angle X-ray scattering, Langmuir, 27, 9528, 10.1021/la2011937
Warren, 2010, Using polymeric precipitation inhibitors to improve the absorption of poorly water-soluble drugs: a mechanistic basis for utility, J Drug Target, 18, 704, 10.3109/1061186X.2010.525652
Watanabe, 2001, Stability of amorphous indomethacin compounded with silica, Int J Pharm, 226, 81, 10.1016/S0378-5173(01)00776-1
Weiss, 1990, Hypersensitivity reactions from taxol, J Clin Oncol, 8, 1263, 10.1200/JCO.1990.8.7.1263
Weng Larsen, 2009, Critical factors influencing the in vivo performance of long-acting lipophilic solutions: impact on in vitro release method design, AAPS J, 11, 762, 10.1208/s12248-009-9153-9
Weuts, 2005, Physical stability of the amorphous state of loperamide and two fragment molecules in solid dispersions with the polymers PVP-K30 and PVP-VA64, Eur J Pharm Sci, 25, 313, 10.1016/j.ejps.2005.03.012
Weuts, 2003, Evaluation of different calorimetric methods to determine the glass transition temperature and molecular mobility below T(g) for amorphous drugs, Int J Pharm, 259, 17, 10.1016/S0378-5173(03)00233-3
Weuts, 2011, Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: etravirine, J Pharm Sci, 100, 260, 10.1002/jps.22242
White, 1991, An experimental animal model for studying the effects of a novel lymphatic drug delivery system for propranolol, Int J Pharm, 69, 169, 10.1016/0378-5173(91)90221-9
White, 2003, Pre-clinical evaluation of itraconazole nanosuspension for intravenous injection, Toxicol Sci, 72, 51
Wiernik, 1987, Phase I trial of taxol given as a 24-hour infusion every 21 days: responses observed in metastatic melanoma, J Clin Oncol, 5, 1232, 10.1200/JCO.1987.5.8.1232
Williams, 2004, Evaluation of drug physical form during granulation, tabletting and storage, Int J Pharm, 275, 29, 10.1016/j.ijpharm.2004.01.042
Williams HD, Anby MU, Sassene PJ, Kleberg K, Bakala-N'Goma J-C, Calderone M, Jannin V, Igonin A, Partheil A, Marchaud D, and Jule E, et al. (2012b) Toward the establishment of standardized in vitro tests for lipid-based formulations. Part 2. The effect of bile salt concentration and drug loading on the performance of type I, II, IIIA, IIIB, and IV formulations during in vitro digestion. Mol Pharm 9:3286–3300.
Williams, 2012, Toward the establishment of standardized in vitro tests for lipid-based formulations. Part 1. Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations, J Pharmaceutical Sci, 101, 3360, 10.1002/jps.23205
Windbergs, 2010, Two-step solid lipid extrusion as a process to modify dissolution behavior, AAPS PharmSciTech, 11, 2, 10.1208/s12249-010-9395-y
Windheuser, 1963, Effect of various compounds on the rate of thiamine hydrolysis, J Pharm Sci, 52, 557, 10.1002/jps.2600520609
Wissing, 2004, Solid lipid nanoparticles for parenteral drug delivery, Adv Drug Deliv Rev, 56, 1257, 10.1016/j.addr.2003.12.002
Won, 2005, Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process, Int J Pharm, 301, 199, 10.1016/j.ijpharm.2005.05.017
Wondraczek, 2009, Advancing glasses through fundamental research, J Eur Ceram Soc, 29, 1227, 10.1016/j.jeurceramsoc.2008.08.006
Woodcock, 1990, Reversal of the multidrug resistance phenotype with cremophor EL, a common vehicle for water-insoluble vitamins and drugs, Cancer Res, 50, 4199
Wu, 2009, Formation and characterization of solid dispersions of piroxicam and polyvinylpyrrolidone using spray drying and precipitation with compressed antisolvent, J Pharm Sci, 98, 2422, 10.1002/jps.21598
Wu, 2011, Physical and chemical stability of drug nanoparticles, Adv Drug Deliv Rev, 63, 456, 10.1016/j.addr.2011.02.001
Wu, 1998, A new understanding of the relationship between solubility and particle size, J Solution Chem, 27, 521, 10.1023/A:1022678505433
Wulff-Pérez, 2012, Controlling lipolysis through steric surfactants: new insights on the controlled degradation of submicron emulsions after oral and intravenous administration, Int J Pharm, 423, 161, 10.1016/j.ijpharm.2011.12.025
Wulff, 1996, An investigation into the critical surfactant concentration for solid solubility of hydrophobic drug in different polyethylene glycols, Int J Pharm, 142, 189, 10.1016/0378-5173(96)04669-8
Xiong, 2008, Preparation and characterization of intravenously injectable nimodipine nanosuspension, Int J Pharm, 350, 338, 10.1016/j.ijpharm.2007.08.036
Yalkowsky SH (1999) Solubility and Solubilization in Aqueous Media, Oxford University Press, New York.
Yalkowsky, 1972, Solubility of nonelectrolytes in polar solvents, J Pharm Sci, 61, 983, 10.1002/jps.2600610643
Yamashita, 2003, Establishment of new preparation method for solid dispersion formulation of tacrolimus, Int J Pharm, 267, 79, 10.1016/j.ijpharm.2003.07.010
Yamashita, 2011, Solvent shift method for anti-precipitant screening of poorly soluble drugs using biorelevant medium and dimethyl sulfoxide, Int J Pharm, 419, 170, 10.1016/j.ijpharm.2011.07.045
Yang, 2004, Combined effect of SLS and (SBE)(7M)-beta-CD on the solubilization of NSC-639829, Int J Pharm, 269, 141, 10.1016/j.ijpharm.2003.09.001
Yang, 2007, Shell-crosslinked Pluronic L121 micelles as a drug delivery vehicle, Biomaterials, 28, 725, 10.1016/j.biomaterials.2006.09.035
Yang, 2009, A novel mixed micelle gel with thermo-sensitive property for the local delivery of docetaxel, J Control Release, 135, 175, 10.1016/j.jconrel.2009.01.007
Yao, 2005, Thermodynamic properties for the system of silybin and poly(ethylene glycol) 6000, Thermochim Acta, 437, 17, 10.1016/j.tca.2005.06.012
Yeh, 1994, Effect of medium-chain glycerides on physiological properties of rabbit intestinal epithelium in vitro, Pharm Res, 11, 1148, 10.1023/A:1018988832492
Yi, 2008, A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs, Eur J Pharm Biopharm, 70, 439, 10.1016/j.ejpb.2008.05.001
Yokoi, 2005, Effects of sugar ester and hydroxypropyl methylcellulose on the physicochemical stability of amorphous cefditoren pivoxil in aqueous suspension, Int J Pharm, 290, 91, 10.1016/j.ijpharm.2004.11.020
Yoo, 1991, Regulation of hepatic microsomal cytochrome P450IIE1 level by dietary lipids and carbohydrates in rats, J Nutr, 121, 959, 10.1093/jn/121.7.959
Yoo, 2000, Bioavailability of itraconazole in rats and rabbits after administration of tablets containing solid dispersion particles, Drug Dev Ind Pharm, 26, 27, 10.1081/DDC-100100324
Yoshioka, 1999, The effect of excipients on the molecular mobility of lyophilized formulations, as measured by glass transition temperature and NMR relaxation-based critical mobility temperature, Pharm Res, 16, 135, 10.1023/A:1018891317006
Young, 2000, Rapid expansion from supercritical to aqueous solution to produce submicron suspensions of water-insoluble drugs, Biotechnol Prog, 16, 402, 10.1021/bp000032q
Yu, 2011, Intestinal transport of bis(12)-hupyridone in Caco-2 cells and its improved permeability by the surfactant Brij-35, Biopharm Drug Dispos, 32, 140, 10.1002/bdd.745
Yu, 2011, An examination of the potential effect of lipids on the first-pass metabolism of the lipophilic drug anethol trithione, J Pharm Sci, 100, 5048, 10.1002/jps.22702
Yu, 2001, Amorphous pharmaceutical solids: preparation, characterization and stabilization, Adv Drug Deliv Rev, 48, 27, 10.1016/S0169-409X(01)00098-9
Zakir, 2011, Nanocrystallization of poorly water soluble drugs for parenteral administration, J Biomed Nanotechnol, 7, 127, 10.1166/jbn.2011.1234
Zana, 1995, Aqueous surfactant-alcohol systems: a review, Adv Colloid Interface Sci, 57, 1, 10.1016/0001-8686(95)00235-I
Zannou, 2007, Stabilization of the maleate salt of a basic drug by adjustment of microenvironmental pH in solid dosage form, Int J Pharm, 337, 210, 10.1016/j.ijpharm.2007.01.005
Zaslavsky, 1978, Action of surface-active substances of biological membranes. III. Comparison of hemolytic activity of ionic and nonionic surfactants, Biochim Biophys Acta, 510, 151
Zhang, 2007, Efficient co-crystal screening using solution-mediated phase transformation, J Pharm Sci, 96, 990, 10.1002/jps.20949
Zhang, 2006, Self-assembled nanoparticles of poly(lactide)-vitamin E TPGS copolymers for oral chemotherapy, Int J Pharm, 324, 191, 10.1016/j.ijpharm.2006.06.013
Zhao, 2011, Prediction of the thermal phase diagram of amorphous solid dispersions by Flory-Huggins theory, J Pharm Sci, 100, 3196, 10.1002/jps.22541
Zhou, 2008, Thermodynamics, molecular mobility and crystallization kinetics of amorphous griseofulvin, Mol Pharm, 5, 927, 10.1021/mp800169g
Zhou, 2002, Physical stability of amorphous pharmaceuticals: importance of configurational thermodynamic quantities and molecular mobility, J Pharm Sci, 91, 1863, 10.1002/jps.10169
Zhu, 2002, Preformulation studies for an ultrashort-acting neuromuscular blocking agent GW280430A. I. Buffer and cosolvent effects on the solution stability, Drug Dev Ind Pharm, 28, 135, 10.1081/DDC-120002446
Ziller, 1988, Control of crystal-growth in drug suspensions. 1. Design of a control unit and application to acetaminophen suspensions, Drug Dev Ind Pharm, 14, 2341, 10.3109/03639048809152019
Zimmermann, 2009, Influence of the solid form of siramesine hydrochloride on its behavior in aqueous environments, Pharm Res, 26, 846, 10.1007/s11095-008-9783-0
Zimmermann, 2000, Influence of different parameters on reconstitution of lyophilized SLN, Int J Pharm, 196, 211, 10.1016/S0378-5173(99)00424-X
Zordan-Nudo, 1993, Effects of nonionic detergents on P-glycoprotein drug binding and reversal of multidrug resistance, Cancer Res, 53, 5994
Zuidema, 1994, Release and absorption rates of intramuscularly and subcutaneously injected pharmaceuticals (II), Int J Pharm, 105, 189, 10.1016/0378-5173(94)90103-1