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

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The effect of glutathionesulphonic acid (N-(N-γ-L-glutamyl-L-β-sulphoalanylglycine, GSO_3H), which is one of the minor metabolites of glutathione(GSH), on the pharmacokinetics of verapamil hydrochloride(verapamil-HCl) and tegafur was investigated in rats. GSO_3H was concomitantly used as sodium salt(GSO_3Na). No significant change by the concomitant use of GSO_3Na was recognized in the pharmacokinetics parameters of verapamil・HCl and tegafur, and plasma elimination of both substances was not affected by GSO_3Na. The tissue-to-plasma concentration ratio(K_p)of verapamil・HCl in the lung 5 min after its administration under concomitant use of GSO_3Na 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 K_p of tegafur under a steady state concentration of GSO_3Na 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 GSO_3Na was related to the increase of the K_p value of verapamil・HCl in the lung. The partition coefficient of GSO_3Na itself decreased when it was used concomitantly with verapamil・HCl.
公益社団法人日本薬学会の論文
2001-04-01