Study on Glutathionesulphonic Acid as Biodistribution Promoter: Concomitant Use Effect on Verapamil Hydrochloride and Tegafur

The effect of glutathionesulphonic acid (N-(N-γ-L-glutamyl-L-β-sulphoalanylglycine, GSO3H), which is one of the minor metabolites of glutathione (GSH), on the pharmacokinetics of verapamil hydrochloride (verapamil·HCl) and tegafur was investigated in rats. GSO3H was concomitantly used as sodium salt...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2001, Vol.24(4), pp.378-384
Main Authors: OHKAWA, Yusuke, HIGASHIYAMA, Kyohko, SUGAYA, Shigenari, ASOH, Tomoyuki, MAEDA, Hiroshi, SASAKI, Kenji, NAKAYAMA, Taiji
Format: Article
Language:English
Subjects:
Animals
Antiarythmic agents
Antimetabolites, Antineoplastic - chemistry
Antimetabolites, Antineoplastic - pharmacokinetics
Antineoplastic agents
biodistribution promoter
Biological and medical sciences
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - pharmacokinetics
Cardiovascular system
Chemotherapy
Chromatography, High Pressure Liquid
concomitant use
drug/metabolite interaction
Glutathione - analogs & derivatives
Glutathione - chemistry
Glutathione - pharmacology
glutathionesulphonic acid
Male
Medical sciences
Pharmacology. Drug treatments
Protein Binding - drug effects
Rats
Rats, Wistar
tegafur
Tegafur - chemistry
Tegafur - pharmacokinetics
Tissue Distribution - drug effects
Verapamil - chemistry
Verapamil - pharmacokinetics
verapamil hydrochloride
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Summary:The effect of glutathionesulphonic acid (N-(N-γ-L-glutamyl-L-β-sulphoalanylglycine, GSO3H), which is one of the minor metabolites of glutathione (GSH), on the pharmacokinetics of verapamil hydrochloride (verapamil·HCl) and tegafur was investigated in rats. GSO3H was concomitantly used as sodium salt (GSO3Na). No significant change by the concomitant use of GSO3Na was recognized in the pharmacokinetics parameters of verapamil·HCl and tegafur, and plasma elimination of both substances was not affected by GSO3Na. The tissue-to-plasma concentration ratio (Kp) of verapamil·HCl in the lung 5 min after its administration under concomitant use of GSO3Na rose significantly, however, this effect disappeared 120 min after administration. No significant change was recognized in other organs. On the other hand, a significant difference of Kp of tegafur under a steady state concentration of GSO3Na was not recognized in any organs. It seemed that the elevation of a lipid solubility (oil water partition coefficient) of verapamil·HCl by the concomitant use of GSO3Na was related to the increase of the Kp value of verapamil·HCl in the lung. The partition coefficient of GSO3Na itself decreased when it was used concomitantly with verapamil·HCl.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.24.378