TY - JOUR
T1 - Study on glutathionesulfonic acid sodium salt as biodistribution promoter for thiopental sodium
AU - Ohkawa, Yuhsuke
AU - Fujimoto, Tomonori
AU - Higashiyama, Kyohko
AU - Maeda, Hiroshi
AU - Asoh, Tomoyuki
AU - Kurumi, Masateru
AU - Sasaki, Kenji
AU - Nakayama, Taiji
N1 - Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2002/6
Y1 - 2002/6
N2 - 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.
AB - 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.
KW - Biodistribution promoter
KW - Concomitant use
KW - Glutathione
KW - Glutathionesulfonic acid sodium salt
KW - Rat
KW - Thiopental sodium
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U2 - 10.1248/bpb.25.761
DO - 10.1248/bpb.25.761
M3 - Article
C2 - 12081143
AN - SCOPUS:0036594102
VL - 25
SP - 761
EP - 765
JO - Biological and Pharmaceutical Bulletin
JF - Biological and Pharmaceutical Bulletin
SN - 0918-6158
IS - 6
ER -