LC-MS-MS方法测定大鼠血浆中蝉翼素的药代动力学及代谢物

Phamacokinetics Study and Its Main Metabolite of Pteryxin in Rats by LC-MS-MS

目的:建立测定蝉翼素血浆药物浓度的液相色谱-电喷雾离子化-质谱(LC-MS-MS)联用的分析方法,探讨其在大鼠体内的药动学及其在体内的代谢产物。方法:大鼠灌胃蝉翼素后不同时间点采血,LC-MS-MS法测定血药浓度,拟合药动学模型并计算相关药动学参数。结果:蝉翼素在0.132 5～53.00μg.L-1线性关系良好(r=0.999 2),方法学考察均符合要求。日内、日间变异系数(RSD)均<10%,精密度和准确度等均符合生物样品分析的要求。结论:该法准确、灵敏、特异,适用于蝉翼素的体内定量分析,蝉翼素在大鼠体内药动学过程属于二室模型,蝉翼素吸收后经过胃肠道转化为代谢产物2-甲基丁酸。

Objective：To develop a LC-MS-MS method to determine pteryxin concentration and its metabolite in rats plasma.Method：Blood samples were collected at different time after oral administration of Peucedunum harry-smithii var subglabrum extract at doses of 80 mg·kg-1.The pteryxin concentration and its metabolite in plasma was determined by LC-MS-MS.Pharmacokinetic parameters were fitted by DAS 2.0 software package.Result： The linear range and the average recovery of pteryxin were 0.132 5-53.00 μg·L-1（r =0.999 2）,and more than 83%（n=5）,respectively.The inner and inter-days precision were both less than 10%.Conclusion： The method described in this report has high sensitivity and selectivity,and was suitable for pharmacokinetic study of pteryxin.The process of pteryin in palsma showed two compartment model after oral administration of Peucedunum harry-smithii var subglabrum extract at doses of 80 mg·kg-1 to rats.