Dự đoán thành viên của lớp độ hòa tan và thẩm thấu: Phân loại BCS tạm thời của những loại thuốc uống hàng đầu thế giới

Dahan A, Amidon GL. Gastrointestinal dissolution and absorption of class II drugs. In: Van de Waterbeemdand H, Testa B, editors. Drug bioavailability: estimation of solubility, permeability, absorption and bioavailability. Weinheim: Wiley-VCH; 2008. p. 33–51. Lennernas H. Human intestinal permeability. J Pharm Sci. 1998;87:403–10. Sun D, Yu L, Hussain M, Wall D, Smith R, Amidon G. In vitro testing of drug absorption for drug ‘developability’ assessment: forming an interface between in vitro preclinical data and clinical outcome. Curr Opin Drug Discov Devel. 2004;7:75–85. Yu LX, Lipka E, Crison JR, Amidon GL. Transport approaches to the biopharmaceutical design of oral drug delivery systems: prediction of intestinal absorption. Adv Drug Deliv Rev. 1996;19:359. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995;12:413. Lobenberg R, Amidon GL. Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur J Pharm Biopharm. 2000;50:3–12. Martinez MN, Amidon GL. A mechanistic approach to understanding the factors affecting drug absorption: a review of fundamentals. J Clin Pharmacol. 2002;42:620–43. Dahan A, Amidon GL. Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Phys Gastro Liver Physiol. 2009;297:G371–7. Kovacevic I, Parojcic J, Homsek I, Tubic-Grozdanis M, Langguth P. Justification of biowaiver for carbamazepine, a low soluble high permeable compound, in solid dosage forms based on IVIVC and gastrointestinal simulation. Mol Pharmaceutics. 2009;6:40–7. Polli J. In vitro studies are sometimes better than conventional human pharmacokinetic in vivo studies in assessing bioequivalence of immediate-release solid oral dosage forms. AAPS J. 2008;10:289–99. Polli J, Abrahamsson B, Yu L, Amidon G, Baldoni J, Cook J, et al. Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond. AAPS J. 2008;10:373–9. Thiel-Demby VE, Humphreys JE, St. John Williams LA, Ellens HM, Shah N, Ayrton AD, et al. Biopharmaceutics classification system: validation and learnings of an in vitro permeability assay. Mol Pharmaceutics. 2009;6:11–8. Yang Y, Faustino PJ, Volpe DA, Ellison CD, Lyon RC, Yu LX. Biopharmaceutics classification of selected beta-blockers: solubility and permeability class membership. Mol Pharmaceutics. 2007;4:608–14. Ahr G, Voith B, Kuhlmann J. Guidances related to bioavailability and bioequivalence: European industry perspective. Eur J Drug Metab Pharmacokinet. 2000;25:25–7. Cook J, Addicks W, Wu Y. Application of the biopharmaceutical classification system in clinical drug development—an industrial view. AAPS J. 2008;10:306–10. Ku M. Use of the biopharmaceutical classification system in early drug development. AAPS J. 2008;10:208–12. Lennernas H, Abrahamsson B. The use of biopharmaceutic classification of drugs in drug discovery and development: current status and future extension. J Pharm Pharmacol. 2005;57:273–85. CDER/FDA. Guidance for industry: waiver of in vivo bioavailability and bioequivalence studies for immediate release dosage forms based on a biopharmaceutical classification system, Center for Drug Evaluation and Research, 2000. Yu LX, Amidon GL, Polli JE, Zhao H, Mehta MU, Conner DP, et al. Biopharmaceutics classification system: the scientific basis for biowaiver extensions. Pharm Res. 2002;19:921. Blume HH, Schug BS. The biopharmaceutics classification system (BCS): class III drugs—better candidates for BA/BE waiver? Eur J Pharm Sci. 1999;9:117. Cheng CL, Yu LX, Lee HL, Yang CY, Lue CS, Chou CH. Biowaiver extension potential to BCS Class III high solubility–low permeability drugs: bridging evidence for metformin immediate-release tablet. Eur J Pharm Sci. 2004;22:297. Jantratid E, Prakongpan S, Amidon GL, Dressman J. Feasibility of biowaiver extension to biopharmaceutics classification system class III drug products: cimetidine. Clin Pharmacokinet. 2006;45:385–99. Stavchansky S. Scientific perspectives on extending the provision for waivers of in vivo bioavailability and bioequivalence studies for drug products containing high solubility-low permeability drugs (BCS-Class 3). AAPS J. 2008;10:300–5. Yamashita S, Tachiki H. Analysis of risk factors in human bioequivalence study that incur bioinequivalence of oral drug products. Mol Pharmaceutics. 2009;6:48–59. Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernas H, Hussain AS, et al. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharmaceutics. 2004;1:85–96. Takagi T, Ramachandran C, Bermejo M, Yamashita S, Yu LX, Amidon GL. A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol Pharmaceutics. 2006;3:631–43. Oh DM, Curl RL, Amidon GL. Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: a mathematical model. Pharm Res. 1993;10:264. Winiwarter S, Ax F, Lennernäs H, Hallberg A, Pettersson C, Karlén A. Hydrogen bonding descriptors in the prediction of human in vivo intestinal permeability. J Mol Graph Model. 2003;21:273–87. Winiwarter S, Bonham NM, Ax F, Hallberg A, Lennernas H, Karlen A. Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. J Med Chem. 1998;41:4939–49. Kim JS, Mitchell S, Kijek P, Tsume Y, Hilfinger J, Amidon GL. The suitability of an in situ perfusion model for permeability determinations: utility for BCS class I biowaiver requests. Mol Pharmaceutics. 2006;3:686–94. WHO list of essential drugs 12th Edition. 2002. http://www.who.int/medicines/organization/par/edl/eml2002core.pdf The top 200 prescriptions for 2002 by number of U.S. prescriptions dispensed.2002. http://www.rxlist.com/top200.htm. Dahan A, Hoffman A. Enhanced gastrointestinal absorption of lipophilic drugs. In: Touitouand E, Barry BW, editors. Enhancement in drug delivery. Boca Raton: CRC press; 2006. p. 111–27. Flanagan SD, Benet LZ. Net secretion of furosemide is subject to indomethacin inhibition, as observed in Caco-2 monolayers and excised rat jejunum. Pharm Res. 1999;16:221–4. Young AM, Audus KL, Proudfoot J, Yazdanian M. Tetrazole compounds: the effect of structure and pH on Caco-2 cell permeability. J Pharm Sci. 2006;95:717–25. Proposal to waive in vivo bioequivalence requirements for the WHO model list of essential medicines immediate release, solid oral dosage forms. http://www.who.int/medicines/services/expertcommittees/pharmprep/QAS04_109Rev1_Waive_invivo_bioequiv.pdf. Lindenberg M, Kopp S, Dressman JB. Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm. 2004;58:265–78. Kim YH, Ramachandran C, Crippen GM, Takagi T, Bermejo M, Amidon GL. In silico approaches to prediction of permeability, solubility and BCS class: Provisional classification of the top-selling IR oral drug products in the United States, Great Britain, Spain, Japan and South Korea In Preparation, 2009. Wuand C-Y, Benet LZ. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res. 2005;22:11–23. Benet L, Amidon GL, Barends D, Lennernäs H, Polli J, Shah V, et al. The use of BDDCS in classifying the permeability of marketed drugs. Pharm Res. 2008;25:483–8. Custodio JM, Wu C-Y, Benet LZ. Predicting drug disposition, absorption/elimination/transporter interplay and the role of food on drug absorption. Adv Drug Deliv Rev. 2008;60:717–33. Chen M-L, Yu L. The use of drug metabolism for prediction of intestinal permeability. Mol Pharmaceutics. 2009;6:74–81. Cao X, Yu LX, Barbaciru C, Landowski CP, Shin HC, Gibbs S, et al. Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability. Mol Pharmaceutics. 2005;2:329–40. Dahan A, Altman H. Food–drug interaction: grapefruit juice augments drug bioavailability—mechanism, extent and relevance. Eur J Clin Nutr. 2004;58:1. Dahan A, Sabit H, Amidon GL. The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J. 2009;11:205–13. Fernández-Teruel C, Nalda Molina R, González-Alvarez I, Navarro-Fontestad C, García-Arieta A, Casabó VG, et al. Computer simulations of bioequivalence trials: selection of design and analyte in BCS drugs with first-pass hepatic metabolism: linear kinetics (I). Eur J Pharm Sci. 2009;36:137–46. Yu LX, Straughn AB, Faustino PJ, Yang Y, Parekh A, Ciavarella AB, et al. The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Mol Pharmaceutics. 2004;1:357–62. Jantratid E, Prakongpan S, Dressman JB, Amidon GL, Junginger HE, Midha KK, et al. Biowaiver monographs for immediate release solid oral dosage forms: cimetidine. J Pharm Sci. 2006;95:974–84. Kalantzi L, Reppas C, Dressman JB, Amidon GL, Junginger HE, Midha KK, et al. Biowaiver monographs for immediate release solid oral dosage forms: acetaminophen (paracetamol). J Pharm Sci. 2006;95:4–14. Manzo RH, Olivera ME, Amidon GL, Shah VP, Dressman JB, Barends DM. Biowaiver monographs for immediate release solid oral dosage forms: amitriptyline hydrochloride. J Pharm Sci. 2006;95:966–73. Polli JE, Yu LX, Cook JA, Amidon GL, Borchardt RT, Burnside BA, et al. Summary workshop report: biopharmaceutics classification system—implementation challenges and extension opportunities. J Pharm Sci. 2004;93:1375–81. Hilfinger JM. BCS in drug discovery, development, and regulation. Mol Pharmaceutics. 2009;6:1–1.