Abstract: 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.

Key words: captopril, captopril, pharmacokinetics, pharmacokinetics, high performance liquid chromatography, high performance liquid chromatography, UV detection, UV detection