Establishing virtual bioequivalence and clinically relevant specifications using in vitro biorelevant dissolution testing and physiologically-based population pharmacokinetic modeling. case example: Naproxen

European Journal of Pharmaceutical Sciences - Tập 143 - Trang 105170 - 2020
Ioannis Loisios-Konstantinidis1, Rodrigo Cristofoletti2, Nikoletta Fotaki3, David B. Turner4, Jennifer Dressman1,5
1Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany
2Center for Pharmacometrics and Systems Pharmacology, Department of Pharmaceutics, College of Pharmacy, University of Florida, Orlando, FL, United States
3Department of Pharmacy and Pharmacology, Faculty of Science, University of Bath, Bath, United Kingdom
4Certara UK Limited, Simcyp Division, 1 Concourse Way, Sheffield, S1 2BJ, United Kingdom
5Fraunhofer IME - Translational Pharmacology and Medicine, Carl-von-Noorden Platz 9, Frankfurt am Main, Germany

Tài liệu tham khảo

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