杀虫双在动物体内的代谢研究 三、杀虫双的高效薄层色谱法测定及其在大鼠体内的毒物代谢动力学研究

本文建立了高效薄层色谱测定大鼠血浆中杀虫双和沙蚕毒素的方法。以甲醇处理血浆样品,取上清液于高效硅胶板上点样,用甲醇-乙酸乙酯(5:4)展开,喷以钙黄绿素-氯化钯溶液,以薄层色谱扫描仪定量测定斑点荧光强度。血浆中加入杀虫双和沙蚕毒素,回收率分别为97.3±2.6％(n=5,CV=2.65％)和94.9±3.9％(n=5,CV=3.92％),检测限杀虫双为11.9ng,沙蚕毒素为5ng。大鼠静脉注射杀虫双后,血浆中立即检出沙蚕毒素。根据开放型二室模型数学公式计算杀虫双及沙蚕毒素代谢动力学各参数值。经口灌胃后,各时相血浆样品中均未检出杀虫双原形。除个别一小时血浆样品中检出低浓度沙蚕毒素外,其他样品中也未检出沙蚕毒素。

Studies on the Metabolism Fate of Shachongshuanq in Animal Ⅲ. High Performance Thin Layer Chromatographic Method and Toxicokinetics of Shachongshuang in Rats

A simple and specific method was established for the determination of Shachongshuang(Ⅰ)and metabolite Nereistoxin(Ⅱ)in plasma by fluorometric HPTLC. The plate was developed with CH_3 OH: CH_3 COOC_2H_5(5: 4), and sprayed with calcein-palladium chloride solution. The detection limit of (Ⅰ) was 11.9ng, and 5 ng for (Ⅱ). (Ⅲ)in plasma was detected immediately after intravenous injection of (Ⅰ). The toxicokinetic parameters of (Ⅰ)and(Ⅱ)calculated respectively according to a 2 compartment open model are as follows. a=5.89, 3.06min~(-1); β=0.11, 0.03min~(-1); t_(1/2α)=0.12, 0.23min; t_(1/2β)=6.49, 21.38min; K_(10)=1.12, 0.14min~(-1); K_(12)=4.31, 2.26min~(-1); K_(21)=0.56, 0.69min~(-1); Vc=30.71, 313.35ml/kg; V_d=322.33, 1409.67 ml/kg; Auc=676.95, 216.91μg, min·ml~(-1); Cl=34.40, 45.11 ml kg~(-1)·min~(-1). There was no (Ⅰ)and only a little(Ⅱ) detected in plasma samples after intragastric administration.