References
- Raoof A , MoriartyD, BraydenDet al. Comparison of methodologies for evaluating regional intestinal permeability. In: In Vitro–In Vivo Correlations. Young D, Devane JG, Butler J(Eds). Plenum, NY, USA (1997).
- Fagerholm U , LindahlA, LennernäsH. Regional intestinal permeability differences in rats of compounds with different physicochemical properties and transport mechanisms. J. Pharm. Pharmacol.49, 687–690 (1997).
- Ungell A -L, Nylander S, Bergstrand S, Sjöberg Å, Lennernäs H. Membrane transport of drugs in different regions of the intestinal tract of the rat. J. Pharm. Sci.87, 360–366 (1998).
- Berggren S , Lennernauml;sP, EkelundM, WeströmB, HoogstraateJ, LennernäsH. Regional transport and metabolism of ropivacaine and its CYP3A4 metabolite PPX in human intestine. J. Pharm. Pharmacol.55, 963–972 (2003).
- Amidon GL , Lennernäs,H, Shah,VP, Crison,JR. A theoretical basis for a biopharmaceutic drug classification, the correlation of in vitro drug dissolution and in vivo bioavailability. Pharm. Res.12, 413–420 (1995).
- Tannergren C , BergendalA, LennernäsH, AbrahamssonB. Toward an increasing understanding of the barriers to colonic drug absorption in humans: implications for early controlled release candidate assessment. Mol. Pharm.6, 60–73 (2009).
- Winkle H . Implementing quality by design. Presented at: PDA/FDA Joint Regulatory Conference. Washington, DC, USA, 24–28 September 2007.
- US FDA. Guidance for Industry. Q8(R2) Pharmaceutical Development. Department of Human and Human Services, Silver Spring, MD, USA (2009).
- US FDA. Guidance for Industry Q10 Quality Systems. Department of Health and Human Services, Silver Spring, MD, USA (2009).
- Selen A , CruañesMT, MüllertzAet al. Meeting report. Applied biopharmaceutics and quality by design for dissolution/release specification setting: product quality for patient benefit. AAPS J. 12, 465–472. (2010).
- Sinko PJ , LeesmanGD, AmidonGL. Predicting fraction dose absorbed in humans using a mass balance approach. Pharm. Res.8, 979–988 (1991).
- Jamei M , TurnerD, YangJet al. Population-based mechanistic prediction of oral drug absorption. AAPS J. 11, 225–237 (2009).
- Agoram B , WoltoszWS, BolgerMB. Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv. Drug Del. Rev.50, S41–S67 (2001).
- Parrott N , LavéT. Applications of physiologically based absorption models in drug discovery and development. Mol. Pharm.5, 760–775 (2008).
- Parrott N , LavéT. Computer models for predicting drug absorption. In: Oral Drug Absorption, Prediction and Assessment, second edition. Dressman JB, Reppas C (Eds). Informa Healthcare, NY, USA (2010).
- Poulin P , JonesRDO, JonesHMet al. PHRMA CPCDC initiative on predictive models of human pharmacokinetics, part 5: prediction of plasma concentration- time profiles in human by using the physiologically-based pharmacokinetic modelling approach. J. Pharm. Sci. 100, 4127–4157 (2011).
- Rowland M , PeckC, TuckerG. Physiologically-based pharmacokinetics in drug development and regulatory science. Ann. Rev. Pharm. Tox.51, 45–73 (2011).
- Sugano K . Introduction to computational oral absorption simulation. Exp. Opin. Drug Metab. Toxicol.5, 259–293 (2009).
- Zhang X , LionbergerRA, DavitBM, YuLX. Utility of physiologically based absorption modelling in implementing quality by design in drug development. AAPS J.13, 59–71 (2011).
- Bolger MB , FraczkiewiczR, LukacovaV. Simulation of absorption, metabolism and bioavailability. In: Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability. Methods and Principles in Medicinal Chemistry (2nd Edition). van der Waterbeemd H, Lennernäs H, Artusson P (Eds). Wiley-VCH, Weinheim, Germany (2009).
- Lukacova V , WoltoszWS, BolgerMB. Prediction of modified release pharmacokinetics and pharmacodynamics from in vitro, immediate release and intravenous data. AAPS J.11, 323–334. (2009).
- Jiang W , KimS, ZhangXet al. The role of predictive biopharmaceutical modelling and simulation in drug development and regulatory evaluation. Int. J. Pharm. 418, 151–160 (2011).
- Watson KJ , DavisJ, JonesHM. Application of physiologically based pharmacokinetic modelling to understanding the clinical pharmacokinetics of UK-369003. Drug Met. Disp.39, 1203–1213 (2011).
- Reddy MD , ConnorA, BrennanBJet al. Physiological modelling and assessments of regional drug bioavailability of danoprevir to determine whether a controlled release formulation is feasible. Biopharm. Drug Disp. 32, 261–275 (2011).
- Connor A , KingG, JonesK. Evaluation of human regional bioavailability to assess whether modified release development is feasible. Proc. AAPS Annual Meeting9(Suppl. 2), 724 (2007).
- Zhu L , ChangI, RubinoCet al. Exposure–response analysis of an oral HIV attachment inhibitor BMS-663068 following 8 days of monotherapy in HIV-infected patients. Presented at: 12th International Workshop on Clinical Pharmacotherapy of HIV Therapy. Miami, FL, USA, 13–15 April 2011.
- Heimbach T , Oh D-M, Li LY, Rodríguez-Hornedo N, Garcia G, Fleisher D. Enzyme-mediated precipitation of parent drugs from their phosphate prodrugs. Int. J. Pharm.261, 81–92 (2003).
- Brown JR . Challenges and solutions in the delivery of a prodrug in an oral extended-release delivery system. Presented at: 9th Annual SMI conference on Controlled Release. London, UK, 28–29 March 2012.
- Marathe P , GreenD, BarbhaiyaR, WenY, CrisonJR Timmins P. Use of a pharmacokinetic absorption model and site of absorption studies to design modified release formulations for BCS3 compounds. Presented at: 3rd PharmSciFair meeting. Prague, Czech Republic, 13–17 June 2011.
- Bergstrand M , SöderlindE, ErikssonUG, WeitschiesW, KarlssonMO. A semi-mechanistic modelling strategy to link in vitro and in vivo drug release for modified release formulations. Pharm. Res.29, 695–706 (2012).
- Bergstrand M , SönderlindE, ErikssonUG, WeitschiesW, KarlssonMO. A semi-mechanistic modelling strategy for characterization of regional absorption properties and prospective prediction of plasma concentrations following administration of new modified release formulations. Pharm. Res.29, 574–584 (2012).
- Yu LX , AmidonGL. A compartmental absorption and transit model for estimating oral drug absorption. Int. J. Pharm.186, 119–125 (1999).
- Corrigan O . The biopharmaceutic drug classification and drugs administered in extended release (ER) formulations. In: In Vitro–In Vivo Correlations. Young D, Devane JG, Butler J (Eds). Plenum, NY, USA (1997).
- Edwards CA . Anatomical and physiological basis: physiological factors influencing drug absorption. In: Colonic Drug Absorption and Metabolism. Marcel Dekker, NY, USA (1993).
- Lennernäs H . Modeling gastrointestinal drug absorption requires more in vivo biopharmaceutical data: experience from in vivo dissolution and permeability studies in humans. Curr. Drug Metab.8, 645–657 (2007).
- Huang S -M, Rowland M. The role of physiologically based pharmacokinetic modelling in regulatory review. Clin. Pharm. Ther.91, 542–549 (2012).
- Jönsson S , HenningssonA, EdholmM, SalmonsonT. Role of modelling and simulation: a European regulatory perspective. Clin. Pharmacokinet.51, 69–76 (2012).
- Grillo JA , ZhaoP, BullockJet al. Utiltiy of physiologically-based pharmacokinetic (PBPK) modeling approach to quantitatively predict a complex drug-drug-disease interaction scenario for rivaroxaban during the drug review process: implications for clinical practice. Biopharm. Drug Dispos. 33, 99–110 (2012).
- Lalonde RL , KowalskiKG, HutmacherMMet al. Model-based drug development. Clin. Pharmacol. Ther. 982, 21–32 (2007).
- Simulations Plus, Inc. GastroPlus User‘s Manual (Version 7.0). Lancaster, CA, USA (2010).
Website
- US FDA. Briefing information for the April 13 2010 meeting of the Pharmaceutical Science and Clinical Pharmacology Advisory Committee. www.fda.gov/downloads/AdvisoryCommitees/CommitteesMeetingMaterials/Drugs/oryCommitteeforPharmaceuticalScienceandClinicalPharmacology/UCM207955.pdf