代谢
对N-ethylperfluorooctanesulfonamide（GX-071）的药代动力学和毒代动力学进行了研究，以支持其作为防治红火蚁的杀虫剂的注册。在大鼠和狗口服GX-071后，其血液中检测到了GX-071及其主要代谢物perfluorooctanesulfonamide（GX-071M）。此方法包括通过冷柱注入毛细管气相色谱分离全血乙醚提取物。毛细管气相色谱/质谱用于确认在大鼠静脉注射25mg/kg GX-071后15分钟取样的40微升血液中GX-071和GX-071M的鉴定。将这些化合物从碱性水相提取到二氯甲烷相作为离子对，并用五氟苄基溴衍生化。在大鼠单次口服150mg/kg GX-071后，血液中GX-071和GX-071M的水平再次表明GX-071被广泛代谢为GX-071M。该程序内部标准百分比再现性为GX-071 4.7和2.8，GX-071M为17和21，分别对应于100万分之100和400亿分之17。作者得出结论，GX-071在首次通过肝脏进入系统循环之前会经历显著地代谢。
An investigation of the pharmacokinetics and toxicokinetics of N-ethylperfluorooctanesulfonamide (GX-071), in support of its registration as a pesticide for use against the red imported fire ant, was presented. GX-071 and its major metabolite, perfluorooctanesulfonamide (GX-071M) were identified in the blood of rats and dogs that had been given oral doses of GX-071. This methodology included the separation of an ethyl-acetate extract of whole blood by cold on column injection capillary gas chromatography. Capillary gas chromatography/mass spectrometry was used to confirm the identification of both GX-071 and GX-071M in a 40 microliter sample of blood taken from a rat 15 minutes after administration of an intravenous dose of 25mg/kg GX-071. The compounds were extracted from an alkaline aqueous phase to a methylene chloride phase as ion pairs and derivatized with pentafluorobenzyl-bromide. The levels of GX-071 and GX-071M in the blood of a rat after a single 150mg/kg oral dose of GX-071 again indicated that GX-071 was extensively metabolized to GX-071M. The percent reproducibility of the internal standard of the procedure was 4.7 and 2.8 at 100 parts per million and 17 and 21 at 400 parts per billion for GX-071 and GX-071M, respectively. The authors conclude that GX-071 undergoes significant hepatic metabolism on a first time pass prior to entry into the systemic circulation.
来源:Hazardous Substances Data Bank (HSDB)
