Evaluation and prediction of oral drug absorption and bioequivalence with food-druginteraction |
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| Affiliation: | 1. Laboratory of Drug Metabolism and Pharmacokinetics, Showa Pharmaceutical University, Machida, Tokyo, 194-8543, Japan;2. Kobe City Medical Center General Hospital, Kobe, Hyogo, 650-0047, Japan;1. Laboratory of Molecular Toxicology, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan;2. Non-Clinical Regulatory Science, Applied Research & Operations, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba, Ibaraki, 305-8585, Japan;3. Division of Drug Metabolism and Molecular Toxicology, Graduate School of Pharmaceutical Sciences, Tohoku University, 6-3 Aramaki-Aoba, Aoba-ku, Sendai, 980-8578, Japan;4. Division of Risk Assessment, National Institute of Health Sciences, Tonomachi 3-25-26, Kawasaki-ku, Kawasaki, 210-9501, Japan;1. Laboratory of Biochemistry and Molecular Biology, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, 565-0871, Japan;2. Integrated Frontier Research for Medical Science Division, Institute for Open and Transdisciplinary Research Initiatives, Osaka University, Suita, Osaka, 565-0871, Japan;3. Laboratory of Biochemistry and Molecular Biology, School of Pharmaceutical Sciences, Osaka University, Osaka, 565-0871, Japan;4. Department of Pharmacokinetics and Nonclinical Safety, Nippon Boehringer Ingelheim Co, Ltd, Kobe, Hyogo, 650-0047, Japan;5. Department of Gastroenterology and Hepatology, School of Medicine, Sapporo Medical University, Sapporo, Hokkaido, 060-8556, Japan;6. Laboratory of Functional Organoid for Drug Discovery, National Institutes of Biomedical Innovation, Health and Nutrition, Ibaraki, Osaka, 567-0085, Japan;7. Global Center for Medical Engineering and Informatics, Osaka University, Suita, Osaka, 565-0871, Japan;1. Clinical Pharmacology & Pharmacokinetics, Project Management Dept, Shionogi & Co, Ltd, Osaka, Japan;2. Pharmacokinetics/Pharmacodynamics & Pharmacometrics, Japan Drug Development & Medical Affairs, Eli Lilly Japan K.K, Kobe, Japan |
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| Abstract: | This article reviews the impacts on the in vivo prediction of oral bioavailability (BA) and bioequivalence (BE) based on Biopharmaceutical classification systems (BCS) by the food-drug interaction (food effect) and the gastrointestinal (GI) environmental change. Various in vitro and in silico predictive methodologies have been used to expect the BA and BE of the test oral formulation. Food intake changes the GI physiology and environment, which affect oral drug absorption and its BE evaluation. Even though the pHs and bile acids in the GI tract would have significant influence on drug dissolution and, hence, oral drug absorption, those impacts largely depend on the physicochemical properties of oral medicine, active pharmaceutical ingredients (APIs). BCS class I and III drugs are high soluble drugs in the physiological pH range, food-drug interaction may not affect their BA. On the other hand, BCS class II and IV drugs have pH-dependent solubility, and the more bile acid secretion and the pH changes by food intake might affect their BA. In this report, the GI physiological changes between the fasted and fed states are described and the prediction on the oral drug absorption by food-drug interaction have been introduced. |
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| Keywords: | In vivo predictive dissolution Oral drug Fasted state Fed state Bioavailability Bioequivalence |
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