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目的建立测定阿立哌唑血浆药物浓度的HPLC-UV检测法,研究国产阿立哌唑片在人体的药动学。方法12名健康志愿受试者和14名健康志愿受试者分别单剂量和多剂量po20 mg国产阿立哌唑片,采用HPLC测定给药后不同时间点血浆中阿立哌唑浓度,用DAS1.0(3P97药动学程序Windows升级版)处理经时血药浓度数据,计算主要药动学参数。结果单次口服阿立哌唑片后的主要药动学参数:ρmax为(108.4±22.5)μg.L-1,tmax为(4.9±0.7)h,AUC0~192 h为(5 748.2±874.5)μg.h.L-1,t1/2β为(107.43±29.03)h,CL/F和V/F分别为(3.56±0.55)L.h-1和(261.60±49.14)L。多次口服阿立哌唑片共14 d达稳态,稳态血药浓度期间给药后(4.0±0.9)h达到峰浓度(480.3±126.2)μg.L-1,AUC0~360 h为(38 166.6±13 241.2)μg.h.L-1,t1/2β为(91.0±21.1)h,CL/F和V/F分别为(0.62±0.36)L.h-1和(60.9±43.7)L。结论国产阿立哌唑的血药浓度-时间曲线符合二室开放模型,为今后的合理用药打下基础。
OBJECTIVE To establish a HPLC-UV method for the determination of aripiprazole in plasma and to study the pharmacokinetics of domestic aripiprazole in human. Methods Twelve healthy volunteers and 14 healthy volunteers were treated with single-dose and multiple-dose domestic aripiprazole po20 mg tablets, and the concentrations of aripiprazole in plasma at different time points were determined by HPLC. .0 (3P97 Pharmacokinetics Windows Upgrade) Processing of blood concentration data over time, calculate the main pharmacokinetic parameters. Results The main pharmacokinetic parameters after a single oral administration of aripiprazole were as follows: 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 / L and 1 / 2β were 107.43 ± 29.03 h and 3.56 ± 0.55 Lh-1 and 261.60 ± 49.14 L respectively for CL / F and V / F. Multiple oral aripiprazole tablets reached a steady state for 14 days, and reached a peak concentration (480.3 ± 126.2) μg.L-1 at 4.0 ± 0.9 h after administration (steady-state plasma concentration) 38.66 ± 13.21.2 μg.hL-1, t1 / 2β was (91.0 ± 21.1) h, CL / F and V / F were (0.62 ± 0.36) Lh-1 and (60.9 ± 43.7) L, respectively. Conclusion The plasma concentration-time curve of domestic aripiprazole conforms to the two-compartment open model, laying a foundation for rational drug use in the future.