Biliary Excretion of Mitomycin C Dextran Conjugates in Relation of Physicochemical Characteristics of Carrier Dextran
スポンサーリンク
概要
- 論文の詳細を見る
Biliary excretion characteristics of polymeric prodrugs of mitomycin C (MMC), mitomycin C-dextran conjugates with cationic or anionic charge (MMC-D_<cat>, MMC-D_<an>) and with different molecular weights of dextran (10000,70000,and 500000) were studied in rat. Following intravenous injection, bile was periodically collected and concentrations of free and dextran-conjugated MMC in it were determined by bioassay. MMC administered as a free from was excreted rapidly into bile and 1.8% of the dose was recovered within 2 h. A small amount of MMC was gradually excreted into bile after administration of all MMC-Ds and total recovery at 8 h was less than 1% of dose. In this case, a major part of excreted MMC was recovered as a conjugated form. MMC-D_<cat> gave a larger total excretion of MMC than MMC-D_<an> and excretion was also affected by the molecular weight of carrier dextran. The biliary recovery of MMC-D_<cat> labeled with ^<14>C at a spacer moiety was significantly higher than that of conjugated MMC determined by bioassay suggesting release and/or inactivation of MMC in MMC-D during the circulation in the body. These results were compared with biliary excretion of model macromolecules with the same molecular weight but different electric charge in order to clarify the effect of electric charge on the biliary excretion of macromolecules. Cationic macromolecules exhibited higher biliary excretion in relation to greater hepatic uptake.
- 社団法人日本薬学会の論文
著者
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Hashida Mitsuru
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Hashida Mitsuru
Faculty Of Pharmaceutical Sciences Kyoto University
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Nishida Koyo
京都大学 薬
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Nishida Koyo
Faculty Of Pharmaceutical Sciences Kyoto University
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Hashida M
Departments Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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ATSUMI Ryo
Faculty of Pharmaceutical Sciences, Kyoto University
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NAKANE Sachi
Faculty of Pharmaceutical Sciences, Kyoto University
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TAKAKURA Yoshinobu
Faculty of Pharmaceutical Sciences, Kyoto University
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SEZAKI Hitoshi
Faculty of Pharmaceutical Sciences, Kyoto University
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Atsumi R
Faculty Of Pharmaceutical Sciences Kyoto University
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Nakane Sachi
Faculty Of Pharmaceutical Sciences Kyoto University
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Sasaki Hitoshi
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Sezaki Hitoshi
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Sezaki Hitoshi
Faculty Of Pharmaceutical Sciences Kyoto University
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Sezaki Hitoshi
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Hashida M
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Takakura Yoshinobu
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Takakura Yoshinobu
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Sasaki H
Nagasaki Univ. School Of Medicine Nagasaki Jpn
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Atsumi Ryo
Faculty Of Pharmaceutical Sciences Kyoto University
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