<原報>ラットにおけるアミノピリンの吸収, 代謝および排泄の速度論的研究

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In the previous report, the pharmacokinetic analyses were carried out in rats for absorption, metabolism and excretion of sulpyrin (S), a watersoluble derivative of aminopyrine (Am), and the effects of differences of dose and administration routes were reported. On this study, Am was analyzed under the same methods as S was investigated, and the results were compared with those of S. After the administration of Am (40 or 100 μmole/head) to rats through various routes (i.v., i.m., p.o.), successive determinations of unchanged Am and its metabolites, 4-monomethylaminoantipyrine, 4-aminoantipyrine, 4-acetylaminoantipyrine, 4-hydroxyantipyrine and its conjugates excreted in urine or bile were carried out. The total recovery rate of unchanged Am and each metabolites excreted in urine after the intravenous injection of Am (40 μmole) was 63%, and the rate of those excreted in bile was only 2.7%. The fact that the urinary excretion rate of unchanged Am and its metabolites after the intravenous injection of Am was lower than that of unchanged S and its metabolites after the intravenous injection of S, which reached 95%, suggested the probability of unknown routes of metabolism and excretion. The increase of the intravenous injection does of Am to 100μmole resulted in the further increase of unknown process. The urinary recovery rate after intramuscular or oral administration of Am (40 μmole) was under 40%. The supposition that the pharmacokinetic behaviors of Am might be complicated made the pharmacokinetic study difficult. The large difference between the elimination rate constant of unchanged Am (0.405hr^<-1>) and that of unchanged S (4.129hr^<-1>) was considered to suggest the relatively long duration of plasma concentration of Am.
共立薬科大学の論文

<原報>ラットにおけるアミノピリンの吸収, 代謝および排泄の速度論的研究

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