HPLC-MS/MS study on determination of rosuvastatin calcium in human plasma and its bioequivalence

Objective:To establish an HPLC-MS/MS method for the determination of rosuvastatin calcium in human plasma,and to study the pharmacokinetics and bioequivalence of rosuvastatin calcium tablets in human volunteers.Methods:A single oral dose of 10 mg test or reference tablets was given to 20 male healthy volunteers in a randomized cross-over design.The concentration of rosuvastatin calcium in plasma was determined by HPLC-MS/MS.Pharmacokinetic parameters were calculated by BAPP 2.0 software.Results:The main pharmacokinetic parameters of test and reference rosuvastatin calcium were as followings:t1/2(7.6±1.0)h and(7.8±1.1)h,tmax(4.0±2.1)h and(4.2±1.6)h,Cmax(15.7±7.8)ng·mL-1 and(16.7±9.4)ng·mL-1,AUC0-72(145±83)ng·mL-1·h-1 and(142±67)ng·mL-1·h-1,AUC0-∞(147±84)ng·mL-1·h-1 and(144±70)ng·mL-1·h-1.The relative bioavailability of test to reference preparation was(102±40)% according to AUC0-72.Conclusion:The method is repeatable and sensitive.The test and reference formulations were bioequivalent.