Pharmacokinetics and Relative Bioavailability of Simvastatin Tablets in Healthy Volunteers

Objective:To establish LC/MS/MS method for determination of Simvastatin in plasma and to study the pharmacokinetics and relative bioavailability following oral administration of trail Simvastatin tablets and reference simvastatin tablets in Chinese healthy volunteers.Methods:Eighteen volunteers were randomly divided into 2 groups.A LC-MS-MS method was used for the determination of Simvastatin in plasma after a single oral dose of 40 mg Simvastatin trail or reference samples in a crossover design.The pharmacokinetic parameters as well as relative bioavailability were analyzed based on a non-compartment model of DAS2.0 statistical software,variation analysis and a two-sided t-test.Results:The main pharmacokinetic parameters of Simvastatin test and reference tablets were as follows:cmax:(9.70±6.62),(10.06±6.29) μg/L;tmax:(1.64±1.01),(1.64±0.68)h;t1/2:(3.48±1.16),(4.15±1.90) h;AUC0～14 h:(29.96±16.28),(32.78±18.53) μg·h·L-1;AUC0～∞ :(31.49±16.65),(36.39±21.71) μg·h·L-1respectively.The relative bioavailability of the test to reference tablets was(97.79±26.63)%.Conclusion:The two preparations are bioequivalent.