吡蚜酮在大鼠体内的毒代动力学研究

采用LC-MS/MS分析方法研究不同染毒剂量下吡蚜酮在SD大鼠体内的毒代动力学特征。色谱柱为Phenomenex Luna C18(50mm×4.6mm,5μm),采用ESI离子源,定量离子对为218.30/105.30。结果表明,大鼠经口灌胃给予吡蚜酮后,由统计矩参数表示的低、高两个剂量组(100mg·kg-1、1 000mg·kg-1)主要毒代动力学参数如下:达峰时间(tmax)分别为4h和2h;峰值浓度(cmax)分别为36 180μg·L-1和69 388μg·L-1;消除半衰期(t1/2β)分别为18.972h和33.177h;表观分布容积(Vz)分别为2.65L·kg-1和8.236L·kg-1;体内总清除率(CLz)分别为:0.107L·h-1·kg-1和0.266L·h-1·kg-1;毒时曲线下面积[AUC(0~t)]分别为652 604.71μg·h·L-1和1 674 767.1μg·h·L-1;AUC(0~∞)分别为931 164.77μg·h·L-1和1 876 484.6μg·h·L-1。在毒性剂量下,吡蚜酮在大鼠体内的毒代动力学过程具有非线性动力学特征。值得注意的是,1 000mg·kg-1剂量组消除半衰期较长,易发生蓄积。该分析方法适用于大鼠血浆中吡蚜酮的测定。

Study on Toxicokinetics of Pymetrozine in Rat

The toxicokinetics process about pymetrozine with different concentrations in rat plasma was in-vestigated by LC-MS/MS.A Phenomenex Luna C18 column（50 mm×4.6 mm,5μm）and ESI ion source were used,and quantitative ion pair was 218.30/105.30.Results showed that,the toxicokinetics parameters of py-metrozine for low and high dosage groups were as follows：tmax was 4 h and 2 h;cmax was 36 180μg·L-1 and 69 388μg·L-1;t1/2βwas 18.972 h and 33.177 h;Vz was 2.65 L·kg-1 and 8.236 L·kg-1;CLz was 0.107 L·h-1 ·kg-1 and 0.266 L·h-1 ·kg-1;AUC（0~t）was 652 604.71 μg·h· L-1 and 1 674 767.1 μg·h· L-1;AUC（0~∞）was 931 164.77 μg·h· L-1 and 1 876 484.6 μg·h· L-1.The toxicokinetics process of py-metrozine in rat plasma possessed the non-linear kinetics characters.It was noticed that pymetrozine with con-centration of 1 000 mg·kg-1 may accumulate easily due to its longer half-life clearance time.The method was suitable for the analysis of concentrations of pymetrozine in rat plasma.