LC-MS法测定菟丝子药材在大鼠血浆中活性成分金丝桃苷的药代动力学研究

Quantitation of Hyperoside in Rat Plasma by LC/MS and Its Application to Pharmacokinetics Study

目的:建立LC-MS分析方法检测大鼠血浆中金丝桃苷浓度,并研究金丝桃苷的药代动力学。方法:5只大鼠单剂量灌胃菟丝子药材提取液,不同时间点采集血浆样品,以淫羊藿苷为内标,采用LC-MS法测定给药后血浆中的药物浓度,并用DAS2.0药代动力学计算程序计算药代动力学参数。结果:金丝桃苷的检测浓度范围在5~200 ng/mL呈线性相关(r=0.999,4),定量限为5 ng/mL。主要动力学参数t1/2为(192.99±124.32)min,Cmax为(63.67±35.58)ng/mL,Tmax为(18.00±8.37)min,AUC0-t为(5,106.80±1,215.15)ng/(min·mL),MRT为(248.83±101.83)min。结论:该法对血浆中金丝桃苷的监测具有专属性,且灵敏、可靠,适用于金丝桃苷的药代动力学研究。

Objective: To establish an LC/MS analytical method to detect the concentration of hyperoside in rat plasma and to study the pharmacokinetics of hyperoside. Methods: 5 rats were given a single dose of Tusizi(Cuscuta) medicinal extract. Plasma samples were collected at different time points. Icariin was used as an internal standard. The drug concentration in plasma was determined by LC/MS method, and the pharmacokinetics parameters were calculated by Das 2.0 pharmacokinetics calculation program. Results: The detection concentration range of hyperoside was linearly in the range of 5-200 ng/mL(r=0.999,4), and the limit of quantification was 5 ng/mL.The main kinetic parameters t1/2 were(192.99±124.32) min, Cmaxwas(63.67±35.58) ng/mL, Tmaxwas(18.00±8.37) min,and AUC0-twas(5,106.80±1,215.15) ng/(min·mL), MRT was(248.83±101.83) min. Conclusion: This method is specific, sensitive and reliable for the monitoring of hyperoside in plasma, which is suitable for the pharmacokinetics study of hyperoside.