6,11-二氢-11-氧代二苯并[be]恶庚英-2-乙酸（异恶草酮）在大鼠、兔、狗、恒河猴和人类体内的处置与代谢的种属差异。
Species differences in the disposition and metabolism of 6,11-dihydro-11-oxodibenz[be]oxepin-2-acetic acid (isoxepac) in rat, rabbit, dog, rhesus monkey, and man.
作者信息
Illing H P, Fromson J M
出版信息
Drug Metab Dispos. 1978 Sep-Oct;6(5):510-7.
The disposition and metabolism of 6,11-dihydro-11-oxodibenz[be]oxepin-2-acetic acid (isoxepac), a new nonsteroidal anti-inflammatory agent, has been studied in rat, rabbit, dog, rhesus monkey, and man. Animals were given single oral or parenteral doses of 5 or 50 mg/kg; man received approximately 3 mg/kg orally. Fecal excretion of radioactivity occurred in the rat (26--37%) and dog (33--49%), whereas in the other species elimination was mainly urinary (less than 83%). Biliary excretion accounted for 18--52% of the dose in the rat and dog. Enterohepatic circulation was demonstrated in both species. Plasma of all species was found to contain mainly unchanged isoxepac. The compound was rapidly eliminated from plasma of dog, rhesus monkey and man, but was more slowly eliminated in rat and rabbit. In the rabbit and dog the principal metabolites were the glycine and taurine conjugates of isoxepac, respectively, whereas in the rhesus monkey and man, isoxepac was excreted unchanged or as the glucuronide.
新型非甾体抗炎药6,11-二氢-11-氧代二苯并[be]氧杂环庚三烯-2-乙酸（异恶草酮）在大鼠、兔、狗、恒河猴和人类中的处置及代谢情况已得到研究。给动物单次口服或肠胃外给予5或50mg/kg的剂量；人类口服约3mg/kg。放射性物质在大鼠（26%-37%）和狗（33%-49%）中经粪便排泄，而在其他物种中消除主要通过尿液（低于83%）。胆汁排泄占大鼠和狗剂量的18%-52%。在这两个物种中均证实存在肝肠循环。所有物种的血浆中主要含有未变化的异恶草酮。该化合物在狗、恒河猴和人类的血浆中迅速消除，但在大鼠和兔中消除较慢。在兔和狗中，主要代谢产物分别是异恶草酮的甘氨酸和牛磺酸共轭物，而在恒河猴和人类中，异恶草酮以未变化形式或葡糖醛酸苷形式排泄。
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