Effect of 5-n-Butyl-1-cyclohexyl-2,4,6-trioxoperhydropyrimidine on the Sulfonamides Transfer in the Rat

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Effect of 5-n-butyl-1-cyclohexyl-2,4,6-trioxoperhydropyrimidine (BCP), an antiinflammatory agent, on the sulfonamide transfer in the rat has been investigated with special attention to the protein binding. Four sulfonamides used in the experiment were sulfamethoxazole, sulfaphenazole, sulfisoxazole, and sulfamethizole. Protein binding and the extent of displacement of a sulfonamide by BCP were studied both in vivo and in vitro techniques using fresh rat plasma. Effect of BCP on the sulfonamides transfer in the rat was investigated in terms of the change of the apparent biological half-life period by the analyses of urinary excretion rate and blood level data. Apparent biological half-life periods of sulfonamides, displaced by BCP to a lesser extent in the in vitro studies, were hardly changed at all, whereas those of sulfonamides, displaced highly by BCP in the same condition, were significantly decreased except sulfamethizole. For the latter compound, it is conceivable that rapid elimination by itself obscures the effect of displacement by BCP. Direct action of BCP on the active renal tubular transport as well as the acetylation of sulfonamides could be ruled out by the apparent lack of the effect of BCP on the accumulation of sulfonamides to the rat kidney cortical slices and the rate of sulfonamide acetylation by acetone powders of the pigeon liver.
社団法人日本薬学会の論文
1970-12-25