Study on glutathionesulfonic acid sodium salt as biodistribution promoter for thiopental sodium

Yuhsuke Ohkawa, Tomonori Fujimoto, Kyohko Higashiyama, Hiroshi Maeda, Tomoyuki Asoh, Masateru Kurumi, Kenji Sasaki, Taiji Nakayama

Research output: Contribution to journalArticle

Abstract

The effects of glutathione (GSH) and glutathionesulfonic acid sodium salt [N-(N-γ-L-glutamyl-L-β-sulfoalanyl)glycine sodium salt, GSO 3Na], which is a minor metabolite of GSH, on the pharmacokinetics of thiopental sodium were investigated in rats. The concomitant use of GSO 3Na with thiopental sodium significantly increased the tissue-to-plasma concentration ratio (Kp) 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 Kp value of thiopental sodium 5 min after its administration with concomitant GSO 3Na decreased significantly only in the spleen. Neither GSO 3Na 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 GSO 3Na but not by GSH. This phenomenon seemed to be concerned with a mechanism to increase the Kp 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.

Original languageEnglish
Pages (from-to)761-765
Number of pages5
JournalBiological and Pharmaceutical Bulletin
Volume25
Issue number6
DOIs
Publication statusPublished - Jun 1 2002

Keywords

  • Biodistribution promoter
  • Concomitant use
  • Glutathione
  • Glutathionesulfonic acid sodium salt
  • Rat
  • Thiopental sodium

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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