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标题：Effects of 4-Hydroxyantipyrine and Its 4-O-Sulfate on Antipyrine as Biodistribution Promoter
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作者：Yuhsuke OHKAWA ; Miki MATSUMURA ; Yuhji KUROSAKI 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：2001
卷号：24
期号：5
页码：529-534
DOI：10.1248/bpb.24.529
出版社：The Pharmaceutical Society of Japan
摘要：The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine, and its 4-O-sulfate (4-S) on the pharmacokinetics of antipyrine were investigated in rats. Plasma elimination of intravenously administered antipyrine was significantly decelerated under a steady-state concentration of 4-OH but not under that of 4-S. Tissue-to-plasma concentration ratio (K_p) of antipyrine under its steady-state concentration was significantly increased in the brain and heart by the concomitant use of 4-OH, while similar use of 4-S had no effect. The enhancement of the blood-brain barrier (BBB) permeability of antipyrine caused by the concomitant use of 4-OH was believed to be concerned with the increase of the K_p value of antipyrine in the brain. These results suggested that 4-OH could be used as a biodistribution promoter.
关键词：biodistribution promoter;antipyrine;4-hydroxyantipyrine;4-hydroxyantipyrine O-sulfate;concomitant use;drug/metabolite interaction