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大鼠血浆和尿液中异丁普生及其代谢物的测定。

Determination of ibuproxam and its metabolites in the plasma and urine of rats.

作者信息

Orzalesi G, Selleri R, Caldini O, Volpato I, Innocenti F, Colome J, Sacristan A, Varez G, Pisaturo G

出版信息

Arzneimittelforschung. 1977;27(5):1012-5.

PMID:577863
Abstract

The metabolism of 2-(4-isobutylphenyl)-propio-hydroxamic acid (ibuproxam, Ibudros), a new molecule with anti-inflammatory, antipyretic and analgesic activity was studied by its administration orally and rectally to the rat. The analysis, carried out with gas chromatographic method and thin-layer chromatography, showed that the drug is present in blood as 2-(4-isobutylphenyl)-propionic acid (ibuprofen), an anti-inflammatory drug which is commonly used and the metabolites of which are already known. Using the same methods, it was observed that only a few traces of the hydroxamic acid appear in the urines of rats treated with ibuproxam, whilst the ibuprofen metabolite is absent. Therefore, we conclude that the drug ibuproxam changes rapidly into ibuprofen, following afterwards the same known metabolic process as the latter drug.

摘要

通过对大鼠口服和直肠给药,研究了具有抗炎、解热和镇痛活性的新分子2-(4-异丁基苯基)-丙酰异羟肟酸(异丁普生,Ibudros)的代谢情况。采用气相色谱法和薄层色谱法进行分析,结果表明该药物在血液中以2-(4-异丁基苯基)-丙酸(布洛芬)的形式存在,布洛芬是一种常用的抗炎药物,其代谢产物已为人所知。使用相同的方法观察到,在用异丁普生治疗的大鼠尿液中仅出现少量异羟肟酸痕迹,而不存在布洛芬代谢产物。因此,我们得出结论,异丁普生药物迅速转变为布洛芬,随后遵循与后一种药物相同的已知代谢过程。

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