<原報>Sulpyrin 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

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The effect of different administration routes of sulpyrin (S) on absorption, metabolism and excretion after the intravenous, intramuscular and oral administration of S in rats was studied pharmacokinetically in the previous reports. Recently, increased cases of admininstration of S suppository has been seen in the field of pediatrics, the authors administered S to rectum of rat, and compared its absorption, metabolism and excretion with the results obtained from other administration routes in the previous reports. Cacao butter and macrogol were used as suppository base, and the effect of different types of base on the pharmacokinetic behaviors of S was also examined. After the rectal administration of S (40μmole) suppository, the urinary excretion rate of nonmetabolite S decreased to less than one half of that of oral administration, and increased amount of 4-acetylaminoantipyrine correspond to this decreased amount was observed. The elimination rate constants of S markedly varied with kind of bases. With cacao butter base, it was 0.951hr^<-1>, while with macrogol base, it was 2.249hr^<-1>, which approximately corresponded to 2.492hr^<-1>, the value after intramuscular injection. Using convolution method, successive absorption rate of S from rectum was estimated as follows. Absorption was almost entirely carried out after 3.5 hrs in the case of cacao butter base and after 2 hrs in the case of macrogol base. Absorption rate of S was 20% and 22%, respectively, which were about one half of that of oral administration. According to the results above, it was estimated that after the administration of S suppository which used macrogol as base, S was absorbed into plasma at the similar rate to that of intramuscular injection, but because of its low absorption rate, plasma concentration of S did not show a temporal, marked increase as in the case of intramuscular injection. On the other hand, when cacao butter was used as base, nonmetabolite S, 4-monomethylaminoantipyrine and 4-aminoantipyrine were considered to remain in the body longer than in the case of macrogol base.
共立薬科大学の論文
1978-02-26

<原報>Sulpyrin 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

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