Effect of Indinavir on the Intestinal Exsorption of Amprenavir, Saquinavir and Nelfinavir after Intravenous Administration in Rats
スポンサーリンク
概要
- 論文の詳細を見る
To elucidate drug interaction between human immunodeficiency virus (HIV) protease inhibitors (PIs), the effect of indinavir (IDV) on the intestinal exsorption of other HIV PIs, amprenavir (APV), saquinavir (SQV) and nelfinavir (NFV) was investigated in rats using an in situ single perfusion method. IDV in the intestinal perfusate inhibited the exsorption of rhodamine 123 (Rho123), a known P-glycoprotein (P-gp) substrate, from blood into intestinal lumen in a concentration-dependent manner, and the inhibitory potency of 10μ_M IDV in the perfusate was close to that of 10μ_M cyclosporin A (CsA) in the perfusate. Ten μ_M of IDV in the intestinal perfusate also decreased significantly the exsorption clearance of Rho123 after intravenous administration. The IDV concentration in this system was not likely to cause hepatic interaction between HIV PIs, because the plasma IDV concentration was far below its inhibition constants for other HIV PIs in the liver microsomes. Thus, 10μ_M of IDV was chosen to investigate the effect of this inhibition on the exsorption of APV, SQV and NFV. IDV in the intestinal perfusate markedly increased the exsorbed amounts of SQV and NFV but not APV after intravenous administrations. Their exsorption clearances, however, showed only a slight increasing tendency or remained unchanged. These findings suggest that in addition to P-gp inhibition, other factors such as CYP3A inhibition might be important in the drug interaction of IDV with APV, SQV and NFV after intravenous administration in rat small intestine. The results obtained in this study will provide useful information to discuss the interactions among PIs when a double protease therapy is used for in HIV-infected patients.
- 公益社団法人日本薬学会の論文
- 2003-02-01
著者
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TAKADA Kanji
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Nishimura Asako
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Womens College of Liber
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Shibata Nobuhito
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Womens College of Liber
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FUKUMOTO Kyoko
Department of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences
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Takada Kanji
Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.
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Takada K
Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories
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YOSHIKAWA Yukako
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Nishimura A
同志社女子大学 薬学部生物薬剤学
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Takada Kanji
Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories
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Nishimura Asako
Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Doshisha Women's College Of L
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Sugioka Nobuyuki
Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.
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INOUE Yuji
Department of Dermatology, Kumamoto University School of Medicine
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Yamasaki Daisuke
Department Of Biochemistry Graduate School Of Pharmaceutical Sciences Hokkaido University
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Yamasaki Daisuke
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Inoue Y
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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GAO Weihua
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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KAGEYAMA Michiharu
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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TADANO Jun
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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FUKUSHIMA Keizou
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Tadano Jun
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Gao W
Tianjin Univ. Tianjin Chn
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Kageyama M
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Takada K
Kyoto Pharmaceutical Univ. Kyoto Jpn
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Fukumoto Kyoko
Department Of Pharmaceutical Sciences Niigata University Of Pharmacy And Applied Life Sciences
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Fukumoto Kyoko
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Gao Weihua
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Shibata Nobuhito
Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.
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Yoshikawa Yukako
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Fukushima K
大正製薬(株)開発研究所薬物動態研究室
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Inoue Yuji
Department Of Dermatology And Plastic And Reconstructive Surgery Graduate School Of Medical And Phar
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Inoue Yuji
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Shibata Nobuhito
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Women's College of Liberal Arts
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