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大鼠胆汁中溴芬酸葡萄糖苷的分离与鉴定。

Isolation and identification of bromfenac glucoside from rat bile.

作者信息

Kirkman S K, Zhang M Y, Horwatt P M, Scatina J

机构信息

Wyeth-Ayerst Research Drug Safety and Metabolism Division, Princeton, NJ 08543, USA.

出版信息

Drug Metab Dispos. 1998 Jul;26(7):720-3.

PMID:9660857
Abstract

Bromfenac (Duract(R)), a drug approved for pain, was expected to be metabolized by the rat to an acyl glucuronide, a metabolite formed with most compounds of similar structure. During the investigation of metabolite profiles in rat bile following administration of 1 mg/kg iv doses of 14C-bromfenac, an acid-labile metabolite was found that degraded to form 14C-bromfenac. Isolation and characterization of this metabolite indicated that it is an unusual conjugate, bromfenac N-glucoside.

摘要

溴芬酸(商品名Duract(R))是一种已获批准用于止痛的药物,预计在大鼠体内会代谢为酰基葡萄糖醛酸苷,这是一种与大多数结构相似的化合物形成的代谢物。在静脉注射1毫克/千克14C-溴芬酸后,对大鼠胆汁中的代谢物谱进行研究时,发现了一种酸不稳定的代谢物,它会降解形成14C-溴芬酸。对这种代谢物的分离和表征表明,它是一种不寻常的共轭物,即溴芬酸N-葡萄糖苷。

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