Modulation of the Pharmacokinetics of 5'-Deoxy-5-fluorouridine and 5-Fluorouracil in Rats by Oral Co-administration of Acyclothymidine
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概要
- 論文の詳細を見る
The effect of an inhibitor of pyrimidine nucleoside phosphorylase (PyNPase), acyclothymidine (AcyT), on the pharmacokinetics of 5'-deoxy-5-fluorouridine (5'-DFUR) and 5-fluorouracil (5-FU) was investigated in an oral co-administration of 5'-DFUR and AcyT in rats. AcyT increased the maximal plasma concentration (C_<max>) and apparent absorption rate constant (k_a) of 5'-DFUR, as expected, but the increase in AUC (area under the curve) was not significant. It was expected that AcyT would only inhibit the phosphorolytic degradation of 5'-DFUR to 5-FU, but the effect was more evident on the pharmacokinetic parameters of 5-FU than on those of 5'-DFUR. AcyT also increased AUC and C_<max> of 5-FU when orally co-administered with 5-FU. An inhibitory effect of AcyT on the enzymatic degradation of 5-FU in rat liver and intestinal extract was investigated. AcyT inhibited the degradation in intestinal extract but not in the liver. The result suggests that orally administered AcyT affects the pharmacokinetics of 5-FU partly by inhibiting 5-FU degradation in the process of intestinal absorption as well as by acting as an inhibitor of PyNPase.
- 公益社団法人日本薬学会の論文
- 1996-05-15
著者
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FUKUSHIMA Shoji
Department of Pathology, Osaka City University Medical School
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Hamada Akinobu
熊本大学医学部附属病院 薬剤
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Hamada Akinobu
Kumamoto Univ. Hospital Kumamoto Jpn
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Hamada Akinobu
Department Of Pharmacy Kumamoto University Hospital
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NAKANO Masahiro
Department of Physics, Kyoto University
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SANEYOSHI MINEO
Department of Biological Sciences, Teikyo University of Sciences and Technology
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Nakano M
Department Of Information Science University Of Occupational And Environmental Health
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Fukushima Shoji
Faculty Of Pharmaceutical Sciences Kobe-gakuin University
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SHIMIZU Satoshi
Faculty of Pharmaceutical Sciences, Josai University
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KAWAGUCHI Takeo
Faculty of Pharmaceutical Sciences, Josai University
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Nakano M
Department Of Biologicalsciences Teikyo University Of Science And Technology
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Saneyoshi Mineo
城西大学 薬
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Saneyoshi Mineo
Department Of Biological Science Teikyo University Of Science And Technology
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Fukushima Shoji
Department Of Pharmacy Kumamoto University Hospital
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Nakano Masahiro
Department Of Biologicalsciences Teikyo University Of Science And Technology
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川口 健夫
城西大学
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Fukushima Shoji
Department Of Pathology Osaka City University Medical School
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Nakano M
Univ. Occupational And Environmental Health Jpn
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Shimizu Satoshi
Faculty Of Dairy Science Rakuno Gakuen University
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Nakano Masahiro
Deparment Of Physics Kyushu University
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Fukushima Shoji
Department Of Gastroenterological Surgery Osaka City University Graduate School Of Medicine
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