RP-HPLC法测定人血浆中穿琥宁含量及药代动力学研究

RP-HPLC determination and its pharmacokinetic research of dehydroandrograpolide succinate sodium for injection in human plasma

目的:研究穿琥宁在人体内的药代动力学过程并建立人生物样品的高效液相色谱方法。方法:采用液-液萃取的方法从生物样品中提取出穿琥宁后用Diaminsil-C18(2)色谱柱(250 mm×4.6 mm,5μm)柱进行分离,采用的流动相为:乙腈-磷酸盐缓冲液[0.5 g.L-1磷酸二氢钾,用磷酸调节pH至2.5(±0.05)](43∶57,v/v)。结果:穿琥宁在人体内静脉给药200 mg后药代动力学符合二室模型,统计距参数为:Cmax为(9.796±2.306)μg.mL-1、Tmax(1.382±0.231)h、T1/2z(1.678±0.509)h。结论:此方法快捷、灵敏、简便,适合于穿琥宁的药代动力学研究。

Objective：To study the pharmacokinetic of dehydroandrograpolide succinate sodium for injection in human and establish the HPLC method in human plasma.Methods：A validated HPLC method is described for the determination of dehydroandrograpolide succinate sodium for injection in human plasma using a liquid-liquid extraction and ultraviolet（UV） absorbance detection.Result：The extraction recovery of dehydroandrograpolide succinate sodium for injection ranged from 70.040% to 79.465%.The linear range was 0.05-100 μg·mL-1,correlation coefficient r2=0.998.Dehydroandrograpolide succinate sodium for injection pharmacokinetic application with intravenous it in human revealed that dehydroandrograpolide succinate sodium for injection followed two-compartment open model.Cmax/μg·mL-1：9.796±2.306、Tmax/ h ：1.382±0.231、T1/2z/h：1.678± 0.509.Conclusion：The method developed was successfully applied to a simple,rapid,specific and accurate HPLC method for investigation of the pharmacokinetics of dehydroandrograpolide succinate sodium for injection in human.