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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 establish a liquid chromatography-electrospray ionization-mass spectrometry (LC-MS-MS) method for the determination of the plasma concentration of cicadaeine in rats and to explore its pharmacokinetics in vivo and its metabolism in vivo product. Methods: Blood was collected from rats at different time points after intragastric administration of cicadaeine, and the plasma concentration was determined by LC-MS-MS. The pharmacokinetic model was fitted and the relevant pharmacokinetic parameters were calculated. Results: There was a good linear relationship between ching wingin and 0.132 5 ~ 53.00μg.L-1 (r = 0.999 2). The methodological study met the requirements. Day and day, the coefficient of variation (RSD) were <10%, precision and accuracy are in line with biological sample analysis requirements. Conclusion: The method is accurate, sensitive and specific, suitable for in vivo quantitative analysis of sicin-1. The pharmacokinetics of sicilypirin in rats is a two-compartment model. After the siccintin is absorbed, it is converted to metabolites 2 - methyl butyric acid.