COMPARATIVE HEPATIC TRANSPORT OF SULFOBROMOPHTHALEIN AND ITS GLUTATHIONE CONJUGATE IN RATS
スポンサーリンク
概要
- 論文の詳細を見る
The hepatic transport of sulfobromophthalein (BSP) and its glutathione conjugate (BSP-GSH) were compared in rats by pharmacokinetic analysis in an attempt to determine the effect of conjugation on the over-all transfer of BSP from blood into bile. In the control rats, the plasma disappearance of BSP was faster than that of BSP-GSH, while the biliary excretion rate of BSP-GSH was significantly higher than that of BSP for the first 10 min. No significant difference in the total amount excreted in the bile for 4 hr was observed between two dyes. In the rats chronically intoxicated with carbon tetrachloride, typical delays were shown in both the plasma disappearance and the biliary excretion of BSP-GSH. In the control rats, the pharmacokinetic parameters, k_<12> and k_<23> of BSP-GSH were significantly smaller than those of BSP, while k_<34> was significantly greater than those of BSP. In the intoxicated rats, significant decreases were observed in k_<12>, k_<23> and k_<34>. The binding of BSP and BSP-GSH to the Y-fraction prepared from the control and intoxicated rats were studied by equilibrium dialysis. In the control rats, the number of high affinity bindings sites (n_1) of BSP-GSH was significantly smaller than that of BSP, while no significant difference was revealed in the binding constant of the high affinity binding site (K_1). In the intoxicated rats, both n_1 and K_1 of BSP-GSH were significantly smaller than those of the control rats. It was suggested that the glutathione conjugation might not play as the rate-determining step in the over-all hepatic transport of BSP.
- 公益社団法人日本薬学会の論文
著者
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Suyama Akihiko
Faculty Of Pharmaceutical Sciences University Of Tokyo
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HANANO Manabu
Faculty of Pharmaceutical Sciences, University of Tokyo
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AWAZU SHOJI
Faculty of Pharmaceutical Science, University of Tokyo
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Hanano M
Department Of Pharmaceutics College Of Pharmacy Nihon University
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Hanano Manabu
Faculty Of Pharmaceutical Science University Of Tokyo
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Iga Tatsuji
Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department
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Awazu Shoji
Department Of Biopharmaceutics Tokyo College Of Pharmacy:department Of Pharmaceutics Research Center
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Awazu Shoji
Faculty Of Pharmaceutical Sciences University Of Tokyo:(present Address)tokyo College Of Pharmacy
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Awazu Shoji
Faculty Of Pharmaceutical Science University Of Tokyo:(present Address)tokyo College Of Pharmacy
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Awazu S
Department Of Biopharmaceutics Tokyo College Of Pharmacy:department Of Pharmaceutics Research Center
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Iga Tatsuji
Division Of Gastroenterology Department Of Medicine Kurume University School Of Medicine
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