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目的建立简便的测定人血浆中卡托普利血药浓度的高效液相色谱法,研究卡托普利在健康人体中的药动学参数.方法以对溴苯乙酰基溴为紫外衍生化试剂,采用高效液相色谱紫外检测法测定18名健康志愿受试者口服单剂量卡托普利受试制剂和参比制剂(50 mg)后血药浓度.结果卡托普利的血药浓度标准曲线的线性范围为25～1200ng@mL-1,其最低定量限为25ng@mL-1,日内及日间BSD均小于8%.应用所建立的血药浓度检测方法测定18名健康志愿受试者口服单剂量卡托普利受试制剂和参比制剂(50 mg)后血药浓度,并计算药动学参数.结果表明口服受试制剂或参比制剂后的tmax分别为(0.64±0.18)h和(0.82±0.41)h;Cmax分别为(600.2±194.3)ng@mL-1和(582.7±175.3)ng@mL-1;AUC0→8h分别为(1448.5±483.7)ng@h@mL-1和(1389.9±392.5)ng@h@mL-1;AUC0→∞分别为(1869.4±701.6)ng@h@mL-1和(1781.8±615.5)ng@h@mL-1.结论本方法操作便捷,灵敏度高,为血药浓度监测及药代动力学研究提供了方法学基础.“,”Aim To establish a simple high-performance liquid chromatography method for the determination of captopril in human plasma and study the pharmacokinetics of captopril in healthy volunteers. Methods Captopril was stabilizedby forming an adduct with p-bromophenacyl bromide and this adduct in plasma was measured by high-performance liquidchromatography with UV detection following a single oral dose 50 mg of captopril test and reference preparations respectivelygiven to 18 healthy volunteers. Results The standard curve was liner over a range of 25 - 1200 ng@ mL- 1. The quantitativelimit of detection was 25 ng@mL-1 . The RSD of inter- and intra- assay were below 8%. On the basis of elaborated method,single-dose pharmacokinetics in 18 healthy volunteers have been investigated. The comparison of the pharmacokinetic parameters was performed. The pharmacokinetic parameters of test and reference tablets were calculated as follows: tmax were(0.64± 0.18)h and (0.82 ± 0.41)h;Cmax were(600.2 + 194.3)ng@mL-1 and (582.7+ 175.3)ng@mL-1 ;AUC0→8h were(1448.5+483.7)ng@h@mL-1 and (1389.9 ± 392.5)ng@h@mL-1 ;AUC0→∞ were (1869.4 + 701.6)ng@ h@mL-1 and (1781.8 +615.5)ng@h@mL-1 , respectively. Conclusion The improved analytical method for captopril was found to be sensitive,simple and rapid, suitable for application in pharmacokinetic studies and routine determination of numerous samples.