水溶液中における利尿薬の安定性ならびに血清アルブミンとの結合

概要

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Stability of seven diuretics in aqueous solution was examined under the condition of equilibrium dialysis study. It was found that furosemide, ethacrynic acid, and bumetanide were not decomposed and that benzothiadiazine derivatives except hydrochlorothiazide were slightly decomposed in pH 7.4 buffer solution within 120 hr at 5° or 6 hr at 30° or 37°. The hydrolysis of hydrochlorothiazide could not be disregarded. The binding of these diuretics by bovine serum albumin (BSA) was investigated using equilibrium dialysis technique at pH 7.4 and 30°. The mathematical analysis of binding data described by Scatchard was applied, and the binding data of hydrochlorothiazide were corrected using its hydrolysis rate. All the compounds were found to interact with BSA, but a large difference in BSA. binding was recognized among them. Physicochemical properties such as ionic form ratio and hydrophilicity of benzothiadiazine derivatives were found to be related to their BSA binding ability.
社団法人日本薬学会の論文
1978-02-25