Küçükgüzel S Güniz, Küçükgüzel Ilkay, Oral Başak, Sezen Sena, Rollas Sevim
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpaşa, Istanbul, Turkey.
Eur J Drug Metab Pharmacokinet. 2005 Jan-Jun;30(1-2):127-34. doi: 10.1007/BF03226418.
Nimesulide (4-nitro-2-phenoxymethanesulfonanilide) is an atypical NSAID lacking a carboxylic acid moiety. It has a good gastric tolerability due to selective inhibition of COX-2. The study objectives in the present work were to characterize the metabolism of nimesulide in rat plasma at certain time intervals. In vitro studies were also carried out to examine if nitroreduction takes place in vitro using rat hepatic subcellular fractions (microsomal and S9 fraction) besides aromatic hydroxylation. This communication describes detection and characterization of nimesulide metabolites isolated from plasma and hepatic subcellular post-incubates by the use of HPLC-UV/diode array and LC-MS/MS. Hydroxynimesulide was the major metabolite both in vivo and in vitro whereas nitroreduction was observed only in vitro with subcellular fractions under anaerobic conditions.
尼美舒利（4-硝基-2-苯氧基甲磺酰苯胺）是一种不含羧酸部分的非典型非甾体抗炎药。由于对COX-2的选择性抑制，它具有良好的胃耐受性。本研究的目的是在特定时间间隔内表征尼美舒利在大鼠血浆中的代谢情况。还进行了体外研究，以检查除芳香族羟基化外，使用大鼠肝脏亚细胞组分（微粒体和S9组分）在体外是否发生硝基还原。本通讯描述了通过使用HPLC-UV/二极管阵列和LC-MS/MS从血浆和肝脏亚细胞孵育后样品中分离出的尼美舒利代谢物的检测和表征。羟基尼美舒利是体内和体外的主要代谢物，而仅在体外厌氧条件下的亚细胞组分中观察到硝基还原。
