Evaluation of Factors to Decrease Plasma Concentration of an HIV Protease Inhibitor, Saquinavir in Ethanol-Treated Rats(Biopharmacy)
スポンサーリンク
概要
- 論文の詳細を見る
Although alcohol consumption is a factor in which the bioavailability of saquinavir (SQV) are retarded, the cause for this phenomenon remains to be uncertain. In the presence study, we examined factors to decrease plasma concentration of SQV in ethanol-treated rats. The ethanol-treated rats were prepared by making them freely access to 15% ethanol solution for 14 d (Day 14 rats). The exsorption clearance of SQV from the blood circulation to the jejunal lumen in the Day 14 rats increased by 6-fold as compared to ethanol non-treated (NT) rats. In the presence of 25 μM ketoconazole (KCZ) or 10 μM cyclosporin A (CsA) in the jejunal lumen, the plasma concentration of SQV in the portal vein increased significantly, and this effect of 10 μM CsA was superior to that of 25 μM KCZ. The biliary excretion clearance of SQV in Day 14 rats also increased by 1.8-fold as compared to that in the NT rats. The metabolic clearance rate (V_<max>/K_m) of SQV in the intestinal microsomes from the Day 14 rats increased significantly, while in the liver microsomes the V_<max>/K_m did not change. The phase II metabolism processes in the Day 14 rats based on UDP-glucuronosyltransferases and gultathion-S-tnrasferase activities were activated, however, they were not likely to be one of factors to decrease the bioavailability of oral SQV, because CYP3A activity in the liver and intestine was not activated to such an extent and SQV itself was not conjugated. These observations suggest that a main possible factor to explain the reducing effect on the SQV oral bioavailability during ethanol consumption is an enhanced efflux of SQV at the intestine and liver, where it is suggested that functional enhancement or excessive expression of P-glycoprotein is caused by ethanol consumption.
- 公益社団法人日本薬学会の論文
- 2004-02-01
著者
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TAKADA Kanji
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Shibata Nobuhito
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Womens College of Liber
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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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KIMURA Keisuke
Department of Internal Medicine, Iwanai Kyokai Hospital
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YOSHIKAWA Yukako
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Kimura Keisuke
Department Of Applied Chemistry Faculty Of Science And Industry Chuo University
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Takada Kanji
Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories
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Sugioka Nobuyuki
Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.
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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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Tadano Jun
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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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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HUKUSHIMA Hiroto
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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NAMIKI Hitomi
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Shibata Nobuhito
Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.
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Namiki Hitomi
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Yoshikawa Yukako
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Kimura Keisuke
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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Hukushima Hiroto
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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