Lisinopril is one of the angiotensin-converting enzyme inhibitors, which have been used for treatment of hypertension and heart failure. The aim of this study was to evaluate the bioequivalence of two lisinopril tablet, $Lisihexal^{circledR}$ and $Zestril^{circledR}$ as a test and reference, respectively. The study was came out on 28 healthy male Korean volunteers in $2{ imes}2$ crossover design. An analytical method with LC-MS-MS was developed for the quantification of lisinopril and enalapril(IS) using SPE method. The condition was selective, sensitive and precise in human plasma, that was enough for the pharmacokinetic study of lisinopril. The pharmacokinetic parameters such as $AUC_t,;AUC_{inf},;C_{max},;T_{max};and;t_{1/2}$ were calculated and ANOVA test was used for the statistical analysis of the parameters using log transformed $AUC_t,;AUC_{inf};and;C_{max}$. $t_{1/2}$ of test and reference drugs were calculated $11.4{pm}5.1;and;16.1{pm}9.9;hr$, respectively. The 90% confidence intervals of $AUC_t,;AUC_{inf};and;C_{max}$ were log 0.9245$sim$log 1.0603, log 0.9270$sim$log 1.0601 and log 0.9548$sim$log 1.1009, within the acceptable range of log 0.8 to log 1.25 by KFDA bioequivalence criteria. Two medications of lisinopril were evaluated bioequivalent and thus may be prescribed interchangeably.