Abstract: AIM: To establish a LC-MS MS method for determination of simvastatin in human plasma, and investigate the pharmacokinetics and bioequivalence of simvastatin tablet in Chinese healthy volunteers.METHODS: 20 male healthy volunteers were randomized to receive a single crossover oral dose of simvastatin reference tablet or domestic tablet.The concentration of simvastatin in plasma was determined by LC-MS/MS.RESULTS: The main pharmacokinetic parameters of test and reference simvastatin tablets were as following:Tmax:1.8 ±1.3,2.10 ±1.00 h, Cmax:7.12 ±1.61, 7.38 ± 1.54μg·L^-1 , AUC(0-24):30.50 ±11.25, 30.17 ±10.21μg·h·L^-1 , t_1/2 :3.90 ±0.78, 3.76 ±0.85 h, respectively.F (0-24) was (101.2 ±7.8) %.CONCLUSION: The assay method is shown to be sensitive and accurate giving reliable results.The test tablet was bioequivalent to the reference tablet.

Key words: simvastatin, LC-MS MS, pharmacokinetics, bioequivalence