Aminopyrine 坐剤投与後のラット尿中排泄物についての速度論的研究

概要

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The effect of different administration routes of aminopyrine (Am) on absorption, metabolism and excretion after the intravenous, intramuscular and oral administration of Am in rats was studied pharmacokinetically in the previous report. In the present report, Am and its metabolites, 4-monomethylaminoantipyrine, 4-aminoantipyrine (AA) and 4-acetylaminoantipyrine excreted in urine were successively determined after the administration of Am to rectum of rat as a suppository. Based on these data, the pharmacokinetic behaviors of Am were discussed comparing with the results of the previous report. Cacao butter and macrogol were also used as suppository base, and the effect of different types of base on the pharmacokinetic behavior of Am was examined. In the case of Am suppository in which cacao butter was used as base, the total recovery of Am and its metabolites from urine was about 21%. In the case of macrogol, it reached 58%, which was slightly higher than the value of 54%, obtained after the intravenous injection of Am. Since the total amount of the urinary excretion of Am and AA, which are said to be effective, was about three times as much when macrogol was used, it is estimated to be more effective to use macrogol as suppository base.
共立薬科大学の論文
1979-02-25