阿立哌唑在中国精神分裂症病人体内的多剂量药动学研究

 目的研究阿立哌唑在中国精神分裂症病人体内的多剂量药动学。方法11名男女精神分裂症病人口服阿立哌唑10mgbid,连用19d后停药,采集血样,用HPLC-MS/ESI测定体内阿立哌唑的血药浓度。采用3P97程序进行数据处理。结果阿立哌唑的稳态药动学参数分别为:t_max(2.6±1.1)h,ρ^ss_min(388.4±108.7)μg·L^-1,ρ^ss_min(557.3±135.5)μg·L^-1,AUC^ss_O-12(5492±1390)μg·h·L^-1,AUC^ss_0-∞(38678±12639)μg·h·L^-1,V_β/F(173±48)L,CL/F(1.9±0.5)L·h^-1,t_1/2β(62.2±9.0)h,MRT(84.5±11.2)h。结论阿立哌唑口服给药后吸收快,分布广,在中国精神分裂症病人体内的血药浓度-时间数据符合一级吸收二室模型。

Pharmacokinetic Study of Aripiprazole in Chinese Schizophrenes Following Multiple Oral Administration

OBJECTIVE To investigate the pharmacokinetics of aripiprazole in Chinese schizophrenes following multiple oral administration.METHODS In an open, randomized study,eleven subjects received 10 mg aripiprazole orally twice a day for 19 d and blood samples were taken for analysis. RESULTS The steady state pharmacokinetic parameters of aripiprazole following 20 mg administration were as follows:t_max(2.6±1.1) h,ρ^ss_max(388.4±108.7)μg·L^-1,ρ^ss_max(557.3±135.5)μg·L^-1,AUC^ss_0-12(5 492±1 390)μg·h·L^-1,AUC^ss_0-∞(38 678±12 639)μg·h·L^-1,V_c/F(173±48)L,CL/F(1.9±0.5)L·h^-1,t_1/2β(62.2±9.0)h,MRT(84.5±11.2)h。CONCLUSION This study obtains the pharmacokinetic parameters of aripiprazole in Chinese schizophrenes.Aripiprazole is well absorbed after oral administration and broadly distributed.The plasma concentration-time profiles of aripiprazole at the dosage of 20 mg in patients are discribed by a two-compartment model with first order absorption.