文章基本信息

标题：Absorption of Methochlorpromazine in Rat Small Intestinal Everted Sac
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作者：Shuji KITAGAWA ; Katsuya SATO ; Shinji SATO 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1996
卷号：19
期号：7
页码：998-1000
DOI：10.1248/bpb.19.998
出版社：The Pharmaceutical Society of Japan
摘要：The absorption of methochlorpromazine in rat small intestinal everted sac was investigated. 0.22% of the drug added in mucosal fluid was transferred to serosal fluid for 30 min at 37°C. The absorption of the drug was slightly inhibited by choline, and more markedly inhibited by more hydrophobic quaternary ammonium cations such as tetraethylammonium and cetyltrimethylammonium. Moderate inhibition was observed by a polyamine, spermine. The absorption rate of methochlorpromazine markedly depended on temperature. The Arrhenius plot of the apparent transfer rate constant revealed high activation energy (117 kJ/mol) for the transport. Uptake of methochlorpromazine to a small intestinal segment was also inhibited by other quaternary ammonium cations corresponding with their inhibitory effects on its transport. These results suggest that methochlorpromazine binds to the relatively hydrophobic region of small intestinal epithelial cells and transfers by passing through a high energy barrier.
关键词：methochlorpromazine;absorption;small intestine;everted sac;rat;quaternary ammonium