A New Pharmacokinetic Model Including in Vivo Dissolution and Gastrointestinal Transit Parameters
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概要
- 論文の詳細を見る
When dissolution is the rate-limiting step in absorption of a drug, both it and gastrointestinal transit can play dominant roles in determining absorption. Therefore, a pharmacokinetic model including the process of dissolution, gastrointestinal transit rate and gastrointestinal pH profile was proposed to explain the behavior of drug formulations in vivo. Clarithromycin (CAM), which exhibits pH-dependent solubility and has high partition coefficients, was used as a drug to test the model, and the effect of a meal on serum concentrations of CAM after a single oral administration to healthy volunteers was evaluated. The results of pharmacokinetic analyses of serum concentration-time data for a single oral administration of CAM to humans in the fasting and postprandial states were well fitted by the new pharmacokinetic model. By substituting the pharmacokinetic parameters obtained into the model equations, the in vivo rate of dissolution could be determined. Pharmacokinetic parameters affecting drug bioavailability were also examined using the model. Factors influencing the behavior of a drug formulation in the gastrointestinal tract were determined. These findings indicate that the model we have proposed can be used to evaluate the behavior of drug formulations in vivo.
- 社団法人日本薬学会の論文
- 1995-06-15
著者
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伊藤 裕二
Department Of Pharmaceutics Research Center Taisho Pharmaceutical Co. Ltd.
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片山 陽子
Department Of Pharmaceutics Research Center Taisho Pharmaceutical Co. Ltd.
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Ito Yoshihisa
College Of Pharmacy Nihon University
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Hayashi H
Drug Research Division Dainippon Sumitomo Pharma Co. Ltd.
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Hayashi Hideya
Pharmaceuticals And Biotechnology Laboratory Japan Energy Corporation
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Hayashi H
Pharmaceuticals & Biotechnology Laboratory Japan Energy Corporation
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石井 邦明
Department of Pharmaceutics, Research Center, Taisho Pharmaceutical Co., Ltd.,
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板井 茂
Department of Pharmaceutics, Research Center, Taisho Pharmaceutical Co., Ltd.,
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林 英文
Department of Pharmaceutics, Research Center, Taisho Pharmaceutical Co., Ltd.,
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Ito Yoshihisa
Res. Unit Of Pharmacology Dep. Of Clinical Pharmacy School Of Pharmacy Nihon Univ. Jpn
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Ito Y
Nihon Univ. Funabashi Jpn
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Itai S
Pharmaceutics Laboratory Medicinal Research Laboratories Taisho Pharmaceutical Co. Ltd.
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Ito Yuji
Otc Product R & D Research Laboratories Taisho Pharmaceutical Co. Ltd.
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板井 茂
Department of Pharmaceutical Engineering and Drug Delivery Science, School of Pharmaceutical Sciences, University of Shizuoka
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