盐酸格拉司琼口腔崩解片的人体生物等效性评价

摘要

Objective: To study the pharmacokinetics of granisetron HCl orally disintegrating tablet and compare its relative bioavailability with domestic granisetron tablet. Methods:Twenty healthy volunteers were administered a single oral dose of domestic granisetron HCl orally disintegrating tablet or tablet(reference) in a randomized crossover study,and their plasma drug concentration was determined by HPLC-fluoremetry. Results: The plasma concentration-time curve was fitted to one-compartment model. The pharmacokinetic parameters obtained were: Cmax = ( 7.2 ± 3.4 ) μg/L, t1/2 = ( 4.2 ± 1.8 ) h, tmax = ( 1.3 ± 0. 3 ) h, AUC0-24 h =(37.3 ± 25.6) μg · h · L. No significant difference was found between the test and the reference groups. The relative bioavailability obtained was(97.9 ± 19.2) ％. Conclusions:The two preparations are bioequivalent.%目的:研究盐酸格拉司琼口腔崩解片的药动学,并与国产盐酸格拉司琼片进行生物利用度比较.方法:20名健康男性志愿者,采用随机交叉给药方案,分别单剂量口服2 mg受试制剂和参比制剂后,采用高效液相色谱荧光法测定血浆药物浓度.结果:健康志愿者单剂量口服盐酸格拉司琼口腔崩解片后体内过程符合开放式血管外一室模型,其Cmax为(7.2±3.4)μg/L,t1/2为(4.2±1.8)h,tmax为(1.3±0.3)h,AUC0~24 h为(37.3±25.6)μg·h·L,与参比制剂的主要药代动力学参数比较,差异均无统计学意义(P>0.05).受试制剂相对于参比制剂的生物利用度为(97.9±19.2)%.结论:两种制剂具有生物等效性.