齐拉西酮片剂的人体药动学

目的:探讨齐拉西酮片剂单剂量口服后药动学。方法:选取9名健康男性受试者,分别口服齐拉西酮片20 mg,于服药后1．0,2．0,3．0,4．0,5．0,6．0,7．0,8．0,9．0,10．0,12．0和14．0 h取静脉血。高效液相色谱法测定齐拉西酮血药浓度,血药浓度数据经3P97程序分析。结果:齐拉西酮血药浓度-时间曲线为一室模型。cmax 为(176±S 86)μg·L-1,tmax为(4．3±0．9)h,t1/2ke为(3．1±1．4)h,Cl为(0．033±0．010)L·h-1,AUC0-14为(705± 247)μg·h·L-1,AUC0-∝为(920±283)μg·h·L-1。结论:9名健康男性受试者口服齐拉西酮片剂20 mg后药动学参数与文献基本一致。

Pharmacokinetics of ziprasidone tablet in healthy subjects

AIM: To study the pharmacokinetics of a single oral dose of ziprasidone in 9 healthy male volunteers. METHODS: A single dose of 20 mg of ziprasidone tablet was administed. The blood samples were taken at 1.0,2.0,3.0,4.0,5.0,6.0,7.0,8.0,9.0,10.0,12.0,14.0 h after oral administration. The concentrations of ziprasidone in serum were determined by HPLC method,the pharmacokinetic parameters were calculated with 3P97 program. RESULTS: The concentration-time curves of ziprasidone fitted to one-comprartment model,with cmax as(176 ± s 86) μg·L-1 ,tmax as(4.3 ± 0.9) h,t1/2ke as (3.1 ± 1.4) h, Cl as (0.033 ± 0.010) L·h-1,AUC0-14 as (705 ± 247) μLg·h·L-1,and AUC0-∝ as (920 ± 283) μg·h·L-1. CONCLUSION: The pharmacokinetic parameters by oral administration ziprasidone 20 rag in 9 healthy male volunteers are similar to report of literature.