西酞普兰片的生物利用度和生物等效性研究

Relative Bioavailability and Bioequivalent of Citalopram Tables in Healthy Volunteers

目的研究国产和进口西酞普兰片在健康男性体内的生物利用度与生物等效性。方法采用双周期交叉实验设计,将18名男性健康受试者随机等分成2组,分别单次口服西酞普兰受试制剂或参比制剂40 mg,在设计的时间点取静脉血。采用高效液相色谱法测定血浆中西酞普兰的浓度,由血药浓度数据获得各自时间曲线下面积(AUC)、峰浓度(Cmax)和达峰时间(Tmax)等药动学参数,以SPSS 10.0软件对主要药动学参数进行方差检验,以t检验进行生物等效性判断。结果西酞普兰片受试制剂组和参比制剂组的AUC0→144、AUC0→∞、Tmax和Cmax分别为1665±318 ng.h/mL和1671±346 ng.h/mL、1806±372 ng.h/mL和1823±405 ng.h/mL、4.6±0.9 h和4.6±1.4 h、34.3±3.8 ng/mL和35.2±4.3 ng/mL。受试制剂对参比制剂的相对生物利用度为100.5%±10.8%。统计学处理表明受试制剂与参比制剂的主要药动学参数之间无明显差异,受试制剂与参比制剂为生物等效制剂。结论受试制剂国产西酞普兰片与参比制剂进口西酞普兰片为生物等效制剂。

Objective To determine the relative bioavailability and bioequivalence of citalopram tablets in the healthy male volunteers. Methods Eighteen healthy male volunteers were equally and ramdomly divided into two groups administered a dose of 40 mg either tested or reference citalopram hydrobromide tablets. The concentration of citalopram hydrobromide in plasma was determined by HPLC. The pharmacokinetic parameters were processed with SPSS 10.0 for variance analysis and two one - side t tests. Results The pharmacokinetic parameters, AUC0→144、AUC0→∞、Tmax and Cmax of the trial preparation or the reference preparation were 1665 ± 318 ng·h/mL and 1671 ± 346 ng·h/mL, 1806 ± 372 ng·h/mL and 1823 ± 405 ng·h/mL,4.6 ± 0.9 h and 4.6 ± 1.4 h,34.3 ± 3.8 ng/mL and 35.2 ± 4.3 ng,/mL respectively. The relative bioavailability was 100.5% ± 10.8%. No significant differences were found among the main pharmacokinetic parameters, and the two one - sided t - tests showed that the trial preparation and the reference preparation were bioequivalent. Conclusion The trial preparation were bioequivalent to the reference preparation.