Abstract: Objective: To evaluate the bioequivalence of lisinopril tablets in healthy volunteers. Methods: A single oral dose of 10 mg test or reference formulations were given to 20 male healthy volunteers in a randomized crossover design. Three ml of blood was drawn out from the ulnar vein of the volunteers at 1, 2 , 3 , 4 , 6 , 8 , 10, 12, 16, 24, 36, 48 and 60 h before and after the administration. The plasma concentration of lisinopril was determined by LC-MS/MS method. The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two formulations. Results: The pharmacokinetic parameters of lisinopril test formulation were obtained as follows:tmax was(6. 1 1. 0) h, Cmax(64. 24 25. 2) g/L, AUC0-60(942. 0 330) g L-1h-1 and AUC0-(969. 6 327) gL-1h-1 ; for reference formulation:tmax was(6. 1 1. 2) h, Cmax(68. 19 26. 5) g/L, AUC0-144(980. 1 340) gL-1h-1 and AUC0-(1002. 3 337) gL-1h-1 . Calculated with AUC0-144 , the bioavailability of the two formulations was(98. 8 27. 5) %. Conclusions: The lisinopril tablet test formulation and reference formulation are bioequivalent.