氢溴酸西酞普兰片的人体药动学及生物等效性研究

目的:比较国产与进口氢溴酸西酞普兰片的人体药动学参数及生物利用度,评价二者的生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服40mg受试制剂(国产)或参比制剂(进口)后,应用高效液相色谱法测定血浆中氢溴酸西酞普兰的浓度,并利用3p97程序计算药动学参数。结果:受试制剂与参比制剂体内药-时曲线符合二室模型,Cmax分别为(147.00±86.04)、(154.13±87.57)ng.mL-1,tmax分别为(4.55±1.35)、(4.75±1.65)h,AUC0～196分别为(6590.69±1866.00)、(7156.26±2181.18)ng.h.mL-1,AUC0～∞分别为(7767.56±2193.92)、(8433.45±2631.88)ng.h.mL-1。受试制剂相对生物利用度为(92.10±18.68)%。结论:受试制剂与参比制剂具有生物等效性。

Pharmacokinetics and Bioequivalence of Domestic Citalopram Hydrobromide Tablet in Healthy Volunteers

OBJECTIVE： To compare the pharmacokinetics and bioavailability between domestic （test） and imported （reference） citalopram hydrobromide tablets and to evaluate the bioequivalence of the two preparations. METHODS： A single dose of 40 mg test tablet or reference tablet of citalopram hydrobromide was administered by randomized crossover way in 20 healthy male volunteers and the plasma concentrations of the citalopram hydrobromide were determined by HPLC. The pharmacokinetic parameters were calculated with 3p97 pharmacokinetic program and the bioavailability was evaluated. RESULTS： The concentration-time curves of two preparations fitted two compartment model. The pharmacokinetic parameters of the test preparation versus the reference preparation were as follows, Cmax： （147.00 ±-86.04）ng · mL^-1 vs. （154.13± 87.57）ng · mL^-1; tmax：（4.55±1.35） h vs（4.75±1.65） h;AUC0-196：（6590.69 ± 1866.00） ng·h·mL^-1 vs.（7156.26±2181.18）ng· h · mL^-1; AUC0-∞： （7 767.56±2 193.92） ng · h · mL^-1 vs.（8 433.45±2 631.88） ng · h · mL^-1. The relative bioavailability of the test citalopram hydrobromide tablet was （92.10 ± 18.68）% . CONCLUSION： The domestic and the reference citalopram hydrobromide tablet are bioequivalent.