Evaluation of Factors to Decrease Bioavailability of Cyclosporin A in Rats with Gentamicin-Induced Acute Renal Failure (Biopharmacy)
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概要
- 論文の詳細を見る
Focusing on the disposition of cyclosporin A (CsA) in the liver and intestine, effects of gentamicin-induced acute renal failure (ARE) on the decreased oral bioavailability of CsA were evaluated in rats. The area under the CsA concentration-time curve (AUC) in ARF rats after oral administration (5 mg/kg) significantly decreased by 43% as compared to the control, while the apparent oral clearance significantly increased by 76% of the control. The portal AUC of CsA in ARF rats with bile flow decreased by 67% as compared to the control rats. Without bile flow, the portal AUC of CsA in control rats decreased by 50% as compared to those with bile flow, whereas ARF rats without bile flow showed no notable change as compared to those with bile flow. The AUC of CsA mono-oxidative metabolite via CYP3A (M-OH) in ARF rats after oral or intravenous administration increased significantly by 84% or 241%, respectively, while there was no difference in the portal M-OH between control and ARF rats, suggesting that the elimination of M-OH was prolonged because of nephrotoxicity. Although the exsorption clearance of CsA from the blood circulation to the intestine after intravenous administration to ARF rats decreased significantly as compared to the control ; and basolateral-to-apical transport of CsA through Caco-2 monolayers was significantly retarded in the presence of uremic toxins, there was no significant change in the total body clearance of CsA between ARF and control rats. Moreover, there were no effects of uremic toxins on the protein binding of CsA in plasma. These observations suggest that hepatic or intestinal CYP3A and P-glycoproteine (P-gp) are not likely to be concerned with lowering the oral bioavailability of CsA, and that bile function under the ARF condition induced by gentamicin is responsible for a marked decrease in the fraction absorbed of CsA in the small intestine.
- 公益社団法人日本薬学会の論文
- 2004-03-01
著者
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FUKUSHIMA Keizo
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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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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Inoue Y
Department Of Pharmacokinetics Kyoto Pharmaceutical University
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SPITELLER Gerhard
Lehrstuhl Organische Chemie I, Universitat Bayreuth
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Spiteller Gerhard
Lehrstuhl Organische Chemie I Universitat Bayreuth
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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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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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