Absorption Characteristics of Macromolecular Prodrugs of Mitomycin C Following Intramuscular Administration
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概要
- 論文の詳細を見る
The absorption characteristics of several kinds of macromolecular compounds following intramuscular injection were studied in rats. Three types of ^<14>C-labeled mitomycin C-dextran conjugates (^<14>C-MMC-D), bare ^<14>C-dextran, ^<14>C-inulin, and ^<131>I-albumin were used, and their absorption and subsequent lymphatic uptake were determined by radioactivity counting. Clearance of cationic ^<14>C-MMC-D from the injection site was slow and varied with the molecular weight. Remarkable accumulation of radioactivity was observed in the regional lymph node after injection of ^<14>C-MMC-D. Bare ^<14>C-dextran showed similar behavior, but the rate of clearance was faster and less accumulation in the lymph node was observed compared with ^<14>C-MMC-D of the same molecular weight. In contrast, ^<14>C-inulin and ^<131>I-albumin showed rapid disappearance from the muscle and no accumulation in the lymph node. Muscular absorption data were fitted to a compartment model including a Langmuir-type absorption. Pharmacokinetic analysis revealed that the rate of absorption and the degree of absorption depended on the molecular weight and electric charge, and MMC-D with a molecular weight of 500000 proved to have the longest period of residence. Thus, it was elucidated that physicochemical properites, such as molecular weight and electric charge, affect the pharmacokinetic behavior of macromolecular compounds injected topically.
- 公益社団法人日本薬学会の論文
- 1986-04-25
著者
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瀬崎 仁
Faculty Of Pharmaceutical Sciences Kyoto University
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瀬崎 仁
京都大学
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高倉 喜信
京都大学大学院薬学研究科病態情報薬学分野
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橋田 充
Faculty Of Pharmaceutical Sciences Kyoto University
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高倉 喜信
Faculty of Pharmaceutical Sciences, Kyoto University
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森 久仁
Faculty of Pharmaceutical Sciences, Kyoto University
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森 久仁
Faculty Of Pharmaceutical Sciences Kyoto University
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