Abstract: AIM　To determine the concentration of fosinoprilat in human plasma and study the pharmacokinetics of fosinopril in healthy Chinese male volunteers following a 20 mg oral dose. METHODS　A liquid chromatographic-mass spectrometric assay has been developed for the determination of fosinopilat in plasma of 10 healthy Chinese male subjects orally administered 20 mg fosinopril. Mobile phase: methanol-acetonitrile-0.1% ammonia water (30∶30∶40); Column: Hewlett Packard Zorbax C₈, 5 μm，15 cm×4.6 mm ID; Flow rate: 0.2 ml.min-1. Selected reaction monitoring(SRM) in mass spectrometric method has been used to detect the characteristic ion of fosinoprilat: m/z 434→m/z 237; internal standard substance enalapril was monitored by full-scan ms2: m/z 375→m/z 105～380. RESULTS　Assay linearity was obtained in the range of 5.0～200.0 ng.mL^-1; Intra- and inter-day precisions were lower than 8.9% and 10.1%, respectively; relative error of the method was lower than 12%. Model-independent pharmacokinetic parameters of fosinoprilat were calculated using Topfit 2.0 software. The main pharmacokinetic parameters were: T_1/2=（6.6±1.2）　h，　T_max=(3.7±1.1)　h，　C_max=(451.9±251.2) ng.mL^-1, AUC_0-∞=(3578.4±2231.2) h。ng。mL^-1. The concentration-time curve of fosinoprilat after an oral dose of fosinopril was not fitted to one-, two- or three-compartment model. CONCLUSION　The values of Tmax, Cmax and AUC_0-∞ obtained here were much higher than those reported for Caucasian, but T_1/2 was significantly lower than that reported. These results offered relevant information for rational use of fosinopril in Chinese subjects.