Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen
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Avdeef, 2007, Solubility of sparingly-soluble ionizable drugs, Adv. Drug Deliv. Rev., 59, 568, 10.1016/j.addr.2007.05.008
Avdeef, 2000, pH-Metric solubility. 2: correlation between the acid-base titration and formulations for use in early animal bioavailability and toxicity studies. later in development, solubility takes on a broader, Pharm. Res., 17, 10.1023/A:1007526826979
Awni, 1995, The pharmacokinetic and pharmacodynamic interactions between the 5-Lipoxygenase inhibitor zileuton and the cyclo-oxygenase inhibitor naproxen in human volunteers, Clin. Pharmacokinet., 29, 112, 10.2165/00003088-199500292-00016
Babiskin, 2015, Application of physiologically based absorption modeling for amphetamine salts drug products in generic drug evaluation, J. Pharm. Sci., 104, 3170, 10.1002/jps.24474
Bergström, 2014, Is the full potential of the biopharmaceutics classification system reached?, Eur. J. Pharm. Sci, 57, 224, 10.1016/j.ejps.2013.09.010
Brown, 2007, Evaluation of cryopreserved human hepatocytes as an alternative in vitro system to microsomes for the prediction of metabolic clearance, Drug Metab. Dispos., 35, 293, 10.1124/dmd.106.011569
Butler, 2010, The developability classification system: application of biopharmaceutics concepts to formulation development, J. Pharm. Sci., 99, 4940, 10.1002/jps.22217
Charles, 1994, Comparative in vitro and in vivo bioavailability of naproxen from tablet and caplet formulations, Biopharm. Drug Dispos., 15, 121, 10.1002/bdd.2510150204
Chowhan, 1978, pH–Solubility profiles of organic carboxylic acids and their salts, J. Pharm. Sci., 67, 1257, 10.1002/jps.2600670918
Cristofoletti, 2013, A comparative analysis of biopharmaceutics classification system and biopharmaceutics drug disposition classification system: a cross-sectional survey with 500 bioequivalence studies, J. Pharm. Sci., 102, 3136, 10.1002/jps.23515
Cristofoletti, 2016, Bridging the gap between in vitro dissolution and the time course of ibuprofen-mediating pain relief, J. Pharm. Sci., 105, 3658, 10.1016/j.xphs.2016.08.024
Cristofoletti, 2016, Differences in food effects for 2 weak bases with similar bcs drug-related properties: what is happening in the intestinal lumen?, J. Pharm. Sci, 105, 2712, 10.1016/j.xphs.2015.11.033
Cristofoletti, 2018, Past, present, and future of bioequivalence: improving assessment and extrapolation of therapeutic equivalence for oral drug products, J. Pharm. Sci., 107, 2519, 10.1016/j.xphs.2018.06.013
Davies, 1997, Clinical pharmacokinetics of naproxen, Clin. Pharmacokinet., 32, 268, 10.2165/00003088-199732040-00002
Dickinson, 2008, Clinical relevance of dissolution testing in quality by design, AAPS J, 10, 380, 10.1208/s12248-008-9034-7
Doki, 2017, Virtual bioequivalence for achlorhydric subjects: the use of pbpk modelling to assess the formulation-dependent effect of achlorhydria, Eur. J. Pharm. Sci., 109, 111, 10.1016/j.ejps.2017.07.035
European Medicines Agency (EMA), 2018a. Committee for medicinal products for human use (CHMP) guideline on the reporting of physiologically based pharmacokinetic (PBPK) modelling and simulation.
European Medicines Agency (EMA), 2018b. Committee for medicinal products for human use (CHMP) guideline on the reporting of physiologically based pharmacokinetic (PBPK) modelling and simulation.
Franssen, 1986, Pharmacokinetics of naproxen at two dosage regimens in healthy volunteers, Int. J. Clin. Pharmacol. Ther. Toxicol., 24, 139
Fruehauf, 2007, Intersubject and intrasubject variability of gastric volumes in response to isocaloric liquid meals in functional dyspepsia and health, Neurogastroenterol. Motil., 19, 553, 10.1111/j.1365-2982.2007.00904.x
Fuchs, 2015, Advances in the design of fasted state simulating intestinal fluids: FaSSIF-V3, Eur. J. Pharm. Biopharm., 94, 229, 10.1016/j.ejpb.2015.05.015
Gøtzsche, 1988, Steady state pharmacokinetics of naproxen in elderly rheumatics compared with young volunteers, Scand. J. Rheumatol., 17, 11, 10.3109/03009748809098754
Grimm, 2018, Interindividual and intraindividual variability of fasted state gastric fluid volume and gastric emptying of water, Eur. J. Pharm. Biopharm., 127, 309, 10.1016/j.ejpb.2018.03.002
Haberer, 2010, Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine, Headache, 50, 357, 10.1111/j.1526-4610.2009.01606.x
Heimbach, T., Laisney, M., Samant, T., Elmeliegy, M., Wu, F., Hanna, I., Lin, W., Zhang, J., Dodd, S., Nguyen-Trung, A.-.T., Tian, H., Vogg, B., Beato, S., Garad, S., Choudhury, S., Ren, X., Mueller-Zsigmondy, M., Einolf, H., Umehara, K., Hourcade-Potelleret, F., He, H.,.PBPK modeling and simulations of oral drug absorption/food effect/ppi /PBIVIVC: Opportunities and challenges dissolution and translational modeling strategies enabling patient-centric product development. 2017.
Heimbach, 2019, Dissolution and translational modeling strategies toward establishing an in vitro-in vivo link—a workshop summary report, AAPS J, 21, 29, 10.1208/s12248-019-0298-x
Hens, 2014, Gastrointestinal transfer: in vivo evaluation and implementation in in vitro and in silico predictive tools, Eur. J. Pharm. Sci., 63, 233, 10.1016/j.ejps.2014.07.008
Jamei, 2009, Population-based mechanistic prediction of oral drug absorption, AAPS J, 11, 225, 10.1208/s12248-009-9099-y
Kambayashi, 2013, Understanding the in vivo performance of enteric coated tablets using an in vitro-in silico-in vivo approach: case example diclofenac, Eur. J. Pharm. Biopharm., 85, 1337, 10.1016/j.ejpb.2013.09.009
Ke, 2016, Towards a best practice approach in pbpk modeling: case example of developing a unified efavirenz model accounting for induction of CYPs 3A4 and 2B6, CPT Pharmacometrics Syst. Pharmacol., 5, 367, 10.1002/psp4.12088
Kuepfer, 2016, Applied concepts in pbpk modeling: how to build a pbpk/pd model, CPT pharmacometrics Syst. Pharmacol., 5, 516, 10.1002/psp4.12134
Lartigue, 1994, Inter- and intrasubject variability of solid and liquid gastric emptying parameters. a scintigraphic study in healthy subjects and diabetic patients, Dig. Dis. Sci., 39, 109, 10.1007/BF02090069
Lennernas, 1995, Human effective permeability data for furosemide, hydrochlorothiazide, ketoprofen and naproxen to be used in the proposed biopharmaceutical classification for IR-products, Pharm. Res. (New York), 12, 396
Lin, 1987, Protein binding as a primary determinant of the clinical pharmacokinetic properties of non-steroidal anti-inflammatory drugs, Clin. Pharmacokinet., 12, 402, 10.2165/00003088-198712060-00002
Loisios-Konstantinidis, 2019, Application of the relationship between pharmacokinetics and pharmacodynamics in drug development and therapeutic equivalence: a pearrl review, J. Pharm. Pharmacol., 71, 699, 10.1111/jphp.13070
Mann, 2017, Validation of dissolution testing with biorelevant media: an orbito study, Mol. Pharm., 14, 4192, 10.1021/acs.molpharmaceut.7b00198
Markopoulos, 2015, In-vitro simulation of luminal conditions for evaluation of performance of oral drug products: choosing the appropriate test media, Eur. J. Pharm. Biopharm., 93, 173, 10.1016/j.ejpb.2015.03.009
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
Mitra, 2019, Maximizing the role of physiologically based oral absorption modeling in generic drug development, Clin. Pharmacol. Ther., 105, 307, 10.1002/cpt.1242
Mooney, 1981, Dissolution kinetics of carboxylic acids I: effect of pH under unbuffered conditions, J. Pharm. Sci., 70, 13, 10.1002/jps.2600700103
Mooney, 1981, Dissolution kinetics of carboxylic acids II: effect of buffers, J. Pharm. Sci., 70, 22, 10.1002/jps.2600700104
Mooney, 1981, Dissolution kinetics of phenylbutazone, J. Pharm. Sci., 70, 1358, 10.1002/jps.2600701218
Niazi, 1996, Dose dependent pharmacokinetics of naproxen in man, Biopharm. Drug Dispos., 17, 355, 10.1002/(SICI)1099-081X(199605)17:4<355::AID-BDD960>3.0.CO;2-N
Obach, 1997, The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data, J. Pharmacol. Exp. Ther., 283, 46
Olivares-Morales, 2016, Development of a novel simplified pbpk absorption model to explain the higher relative bioavailability of the OROS® formulation of oxybutynin, AAPS J, 18, 1532, 10.1208/s12248-016-9965-3
Ozturk, 1988, Dissolution of lonizable drugs in buffered and unbuffered solutions, Pharm. Res., 05, 272, 10.1023/A:1015970502993
Paixão, 2018, Gastric emptying and intestinal appearance of nonabsorbable drugs phenol red and paromomycin in human subjects: a multi-compartment stomach approach, Eur. J. Pharm. Biopharm., 129, 162, 10.1016/j.ejpb.2018.05.033
Paixão, 2012, Prediction of the human oral bioavailability by using in vitro and in silico drug related parameters in a physiologically based absorption model, Int. J. Pharm., 429, 84, 10.1016/j.ijpharm.2012.03.019
Parrott, 2014, Physiologically based absorption modelling to predict the impact of drug properties on pharmacokinetics of bitopertin, AAPS J, 16, 1077, 10.1208/s12248-014-9639-y
Pathak, 1997, Establishment of virtual bioequivalence using population-based pbpk modelling: application to the setting of dissolution limits, AAPS J
Pathak, 2019, Biopharmaceutic IVIVE—Mechanistic modeling of Single- and Two-Phase in vitro experiments to obtain drug-specific parameters for incorporation into PBPK models, J. Pharm. Sci., 108, 1604, 10.1016/j.xphs.2018.11.034
Pepin, X.J.H., Flanagan, T.R., Holt, D.J., Eidelman, A., Treacy, D., Rowlings, C.E., 2016. Justification of drug product dissolution rate and drug substance particle size specifications based on absorption pbpk modeling for lesinurad immediate release tablets.
Pérez, 2004, A topological sub-structural approach for predicting human intestinal absorption of drugs, Eur. J. Med. Chem., 39, 905, 10.1016/j.ejmech.2004.06.012
Petring, 1990, Inter- and intrasubject variability of gastric emptying in healthy volunteers measured by scintigraphy and paracetamol absorption, Br. J. Clin. Pharmacol., 29, 703, 10.1111/j.1365-2125.1990.tb03691.x
Poulin, 2009, Development of a novel method for predicting human volume of distribution at steady-state of basic drugs and comparative assessment with existing methods, J. Pharm. Sci., 98, 4941, 10.1002/jps.21759
Psachoulias, 2011, Precipitation in and supersaturation of contents of the upper small intestine after administration of two weak bases to fasted adults, Pharm. Res., 28, 3145, 10.1007/s11095-011-0506-6
Rao, 1993, Pharmacokinetics of single-dose administration of naproxen at 1O : oo and 22 : oo hours, Int. Soc. Chronobiol., 10, 137, 10.3109/07420529309059703
Rosenberger, 2019, Application of a refined developability classification system, J. Pharm. Sci., 108, 1090, 10.1016/j.xphs.2018.10.044
Runkel, 1972, Absorption, distribution, metabolism, and excretion of naproxen in various laboratory animals and human subjects, J. Pharm. Sci., 61, 703, 10.1002/jps.2600610507
Runkel, 1973, Naproxen-metabolism, excretion and comparative pharmaco kinetics, Scand J Rheumatol, 2, 29, 10.3109/03009747309097093
Runkel, 1972, Naproxen oral absorption characteristics, Chem. Pharm. Bull. (Tokyo), 20, 1457, 10.1248/cpb.20.1457
Darwich, 2010, Interplay of metabolism and transport in determining oral drug absorption and gut wall metabolism: a simulation assessment using the “Advanced dissolution, absorption, metabolism (ADAM)” model, Curr. Drug Metab., 11, 716, 10.2174/138920010794328913
Selen, 2014, The biopharmaceutics risk assessment roadmap for optimizing clinical drug product performance, J. Pharm. Sci., 103, 3377, 10.1002/jps.24162
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
Setiawati, 2009, Bioequivalence study with two naproxen sodium tablet formulations in healthy subjects, J. Bioequivalence Bioavailab. -Open Access Res. Artic. JBB J Bioequiv Availab, 1, 28
Shebley, 2018, Physiologically based pharmacokinetic model qualification and reporting procedures for regulatory submissions: a consortium perspective, Clin. Pharmacol. Ther., 104, 88, 10.1002/cpt.1013
Sheng, 2009, Toward an in vivo dissolution methodology: a comparison of phosphate and bicarbonate buffers, Mol. Pharm., 6, 29, 10.1021/mp800148u
Stillhart, 2017, Characterising drug release from immediate-release formulations of a poorly soluble compound, basmisanil, through absorption modelling and dissolution testing, AAPS J., 19, 827, 10.1208/s12248-017-0060-1
Suarez-Sharp, 2018, Applications of clinically relevant dissolution testing: workshop summary report, AAPS J, 20, 93, 10.1208/s12248-018-0252-3
Tubic-Grozdanis, 2008, Application of gastrointestinal simulation for extensions for biowaivers of highly permeable compounds, AAPS J, 10, 213, 10.1208/s12248-008-9023-x
Upton, 1984, Naproxen pharmacokinetics in the elderly, Br. J. Clin. Pharmacol., 18, 207, 10.1111/j.1365-2125.1984.tb02454.x
Van den Ouweland, 1988, Pharmacokinetics of high-dosage naproxen in elderly patients, Int. J. Clin. Pharmacol. Ther. Toxicol., 26, 143
Vree, 1993, Pharmacokinetics of naproxen, its metabolite O‐desmethylnaproxen, and their acyl glucuronides in humans, Biopharm. Drug Dispos., 14, 491, 10.1002/bdd.2510140605
Wang, 2002, General solution for diffusion‐controlled dissolution of spherical particles. 2. evaluation of experimental data, J. Pharm. Sci, 91, 534, 10.1002/jps.10039
Wang, 1999, General solution for diffusion‐controlled dissolution of spherical particles. 1. theory, J. Pharm. Sci, 88, 731, 10.1021/js980236p
U.S-FDA Center for Drug Evaluation and Research (CDER), 2018b. Physiologically based pharmacokinetic analyses — format and content guidance for industry.
U.S-FDA Center for Drug Evaluation and Research (CDER), 2018a. Physiologically based pharmacokinetic analyses — format and content guidance for industry.
Wedagedera, J., Cain, T., Pathak, S.M., Jamei, M., 2017. Virtual bioequivalence assessment of two tramadol formulations using the advanced dissolution absorption and metabolism (ADAM) model via simcyp R package.
Yazdanian, 2004, The “High solubility” definition of the current fda guidance on biopharmaceutical classification system may be too strict for acidic drugs, Pharm. Res., 21, 293, 10.1023/B:PHAM.0000016242.48642.71
Zhang, 2017, Integrating in vitro , modeling, and in vivo approaches to investigate warfarin bioequivalence. cpt pharmacometrics syst, Pharmacol, 6, 523
Zhao, 2012, Best practice in the use of physiologically based pharmacokinetic modeling and simulation to address clinical pharmacology regulatory questions, Clin. Pharmacol. Ther., 92, 17, 10.1038/clpt.2012.68
Zhao, 2001, Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with Abraham descriptors, J. Pharm. Sci., 90, 749, 10.1002/jps.1031
Zhou, 1998, Single- and multiple-dose pharmacokinetic comparison of a sustained-release tablet and conventional tablets of naproxen in healthy volunteers, J. Clin. Pharmacol., 38, 625, 10.1002/j.1552-4604.1998.tb04469.x