Pharmacokinetics of amlodipine besylate tablets in healthy volunteers

Objective: To develop a sensitive and specific LC-MS-MS method for determination of amlodipine in human plasma and investigate the pharmacokinetics of amlodipine besylate tablets in healthy volunteers.Methods: Twelve male healthy volunteers received single oral dose of amlodipine besylate tablets 10 mg.The plasma concentrations of amlodipine were determined by LC-MS-MS method after liquid-liquid extraction.The pharmacokinetic parameters were calculated by non-compartment model.Results: The calibration curve was linear in the concentration range of 0.501-20.04 ng/mL.The limit of quantification was 0.501 ng/mL.The method was successfully applied to pharmacokinetic study of amlodipine besylate tablets.The main pharmacokinetic parameters of amlodipine were as follows: cmax(9.57±1.08) ng/mL,tmax(5.92±0.79) h,t1/2(30.14±5.46) h,MRT(45.25±6.08) h,Cl/F(40.02±4.98) L/h,AUC0~96(312.78±34.07) ng·h·mL-1 and AUC0~∞(352.09±42.45) ng·h·mL-1.Conclusion:The method is proved to be accurate,sensitive,linear and reproducible for the determination of amlodipine in human plasma.It is suitable for pharmacokinetic study of amlodipine besylate tablets in healthy volunteers.