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Mechanism for drug absorption from rat-liver surface membrane: effect of dose and transport inhibitors on the pharmacokinetics of phenol red


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タイトル: Mechanism for drug absorption from rat-liver surface membrane: effect of dose and transport inhibitors on the pharmacokinetics of phenol red
著者: Nishida, Koyo / Amagishi, Hiroaki / Sasaki, Hitoshi / Nakamura, Junzo
発行日: 1995年 3月
出版者: Pharmaceutical Press
引用: Journal of Pharmacy and Pharmacology, 47 (3), 227-231, 1995
抄録: We examined the effect of dose and transport inhibitors on the pharmacokinetics of phenol red as a model drug after application to rat liver surface in-vivo, employing a cylindrical glass cell (i.d. 9 mm, area 0.64 cm2), to elucidate the mechanism for drug absorption from liver surface membrane. Absorption ratios of phenol red in 6 h were determined to be 91.1, 91.8 and 89.9 % at a dose of 0.3, 1 and 3 mg, respectively. Also, the AUC value for plasma concentration profile of phenol red was proportional to the dose. It is thus suggested that absorption process of phenol red from rat liver surface does not approach saturability. Time course of remaining amount of phenol red in glass cell obeyed the first-order kinetics at a dose of 0.3 mg, and its rate constant Ka was calculated to be 0.0069 min-1. Moreover, no significant difference was seen in Ka value within the dose range of 0.3 - 3 mg, which was estimated by curve fitting of the plasma concentration profile of phenol red after application to rat liver surface in the two-compartment model with first-order absorption. 2,4-Dinitrophenol (0.3 mg) and probenecid (0.5 and 1 mg), inhibitors of metabolic energy and anion transport respectively, had no significant effect on the pharmacokinetics of phenol red after application to rat liver surface. These data demonstrate that specific transport mechanism such as active transport is not involved in phenol red absorption from rat liver surface membrane.
記述: without figures / グラフなし
URI: http://hdl.handle.net/10069/6673
ISSN: 00223573
PubMed ID: 7602486
資料タイプ: Journal Article
原稿種類: author
出現コレクション:050 学術雑誌論文

引用URI : http://hdl.handle.net/10069/6673

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