文章基本信息

标题：Study on Glutathionesulfonic Acid Sodium Salt as Biodistribution Promoter for Thiopental Sodium
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作者：Yuhsuke Ohkawa ; Tomonori Fujimoto ; Kyohko Higashiyama 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：2002
卷号：25
期号：6
页码：761-765
DOI：10.1248/bpb.25.761
出版社：The Pharmaceutical Society of Japan
摘要：The effects of glutathione (GSH) and glutathionesulfonic acid sodium salt [ N -( N -γ- L -glutamyl- L -β-sulfoalanyl)glycine sodium salt, GSO₃Na], which is a minor metabolite of GSH, on the pharmacokinetics of thiopental sodium were investigated in rats. The concomitant use of GSO₃Na with thiopental sodium significantly increased the tissue-to-plasma concentration ratio ( K _p) of thiopental sodium 60 min after its administration in the heart, lung, brain, liver, kidney, and spleen, while GSH did not affect them. On the other hand, the K _p value of thiopental sodium 5 min after its administration with concomitant GSO₃Na decreased significantly only in the spleen. Neither GSO₃Na nor GSH changes the pharmacokinetic parameters of thiopental sodium. Significant change of the binding ratio of thiopental sodium to bovine serum albumin (BSA) was not observed by the addition of less than 5-fold GSO₃Na. About 50% of thiopental sodium was bound to the brain, lung or liver, however, no significant change of this binding ratio was observed by the concomitant use of GSO₃Na. The partition coefficient of thiopental sodium apparently increased by the concomitant use of GSO₃Na but not by GSH. This phenomenon seemed to be concerned with a mechanism to increase the K _p values of thiopental sodium in the tissues. The increment in the drug distribution to tissues with concomitant GSO₃Na observed in this study is useful information for the application of drug combinations as a biodistribution promoter.
关键词：biodistribution promoter;concomitant use;glutathionesulfonic acid sodium salt;glutathione;thiopental sodium;rat