Pharmacokinetics study of aripiprazole tablets in Chinese healthy volunteers

OBJECTIVE To research the pharmacokinetics of aripiprazole in healthy volunteers after administration with single or multiple dose of aripiprazoLe,and compare its gender difference.METHODS In single dose study,6 male and 6 female volunteers received a single dose of 10,20,40 mg aripiprazole tablets,respectively in 3 stages.In multiple dose study,other 6 male and 6 female volunteers administered aripiprazole tablets(20 mg,qd,for 14 days).Aripiprazole concentration in plasma was determined by HPLC.Main pharmacokinetic parameters were calculated and compared by statistic analysis.RESULTS The pharmacokinetic parameters obtained from the single-dose study of 10,20,40 mg were,respectively,as follows:AUC0-t(16 431.8±2 350.5),(40 184.0±5 256.7)and(71 629.1±8 616.5)μg·h·L-1;tmax(4.4±1.3),(4.2±0.8)and(4.3±0.9)h;Cmax(187.2±20.9),(410.1±58.3) and(700.8±143.6) μg·L-1;t1/2,β(83.22±9.43),(75.11±10.06) and(84.17±22.43)h..The steady-state pharmacokinetic parameters were as follows: AUCτss(11961.1±2675.7)μg·h·L-1;tssmax为(4.4±1.2)h;Cssmax(634.2±137.1)μg·L-1;Cssmin(361.3±95.7)μg·L-1;Cav(498.4±111.5)μg·L-1;DF(55.6±7.5) %;t1/2β(66.42±12.65)h.Statistical analysis indicated that there was no gender difference in pharmacokinetic parameters,except of tssmax in multiple dose study.CONCLUSION The concentration-time curves of aripiprazole are fitted to a two-compartment model.In the dose range of 10-40 mg,Cmax and AUC0-t follow the rule of dose-dependant manner.There was no gender difference in the main pharmacokinetic parameters.