Study on Pharmacokinetics of Domestic Aripiprazole After Single and Multiple Dosing in Healthy Volunteers

OBJECTIVE To develop a HPLC-UV method for determining Aripiprazole in human plasma and study the pharmacokinetic profiles of domestic Aripiprazole tablets in healthy volunteers.METHODS A single and multiple oral doses of domestic aripiprazole were given to 12 and 14 healthy volunteers respectively.Aripiprazole concentrations in plasma were determined by HPLC method.The pharmacokinetic parameters of aripiprazole were obtained with statistical analysis by DAS1.0.RESULTS The main pharmacokinetic parameters of a single dose of aripiprazole were as followed:ρmax was (108.4±22.5) μg·L-1,tmax was(4.9±0.7) h,AUC0～192 h was(5 748.2±874.5) μg·h·L-1,t1/2βwas(107.4±29.0)h,CL/F was(3.56±0.55) L·h-1 and V/F was(261.6±49.1) L.In multiple dose study,aripiprazole were given to the healthy volunteers for 14 d to achieve steady state,the peak concentration of(480.3±126.2) μg·L-1 and was reached at(4.0±0.9) h after the last administration in steady state.AUC0～360 h was(38 166.6±13 241.2) μg·h·L-1,t1/2β was(91.0±21.1)h,CL/F was(0.62±0.36) L·h-1 and V/F was(60.9±43.7) L.CONCLUSION The concentration-time curves of aripiprazole were described by a two-compartment open model.And it offered necessary information for clinical use of aripiprazole in Chinese.