盐酸胺碘酮分散片人体生物等效性研究

目的:研究盐酸胺碘酮分散片的人体生物等效性。方法:采用双周期交叉试验设计,18名健康男性受试者随机交叉单剂量口服盐酸胺碘酮分散片(受试制剂)与盐酸胺碘酮片(参比制剂)400mg,采用液-质联用(LC-MS)法测定人血浆中盐酸胺碘酮经-时血药浓度,利用SPSS10.0统计软件计算药动学参数,评价二制剂的生物等效性。结果:受试制剂与参比制剂的tmax分别为(4.2±1.2)、(3.8±0.9)h,Cmax分别为(420.0±211.7)、(414.8±166.7)ng.mL-1,t1/2分别为(38.8±20.4)、(39.6±12.5)h,AUC0～96分别为(6 375.3±3 093.1)、(6 518.4±3 101.1)ng.h.mL-1,AUC0～∞分别为(7 165.3±3 680.2)、(7 325.5±3478.1)ng.h.mL-1。受试制剂中盐酸胺碘酮的相对生物利用度为(98.4±8.4)%。结论:盐酸胺碘酮分散片与盐酸胺碘酮片具有生物等效性。

Bioequivalence of Amiodarone Hydrochloride Dispersible Tablets in Healthy Volunteers

OBJECTIVE： To study the bioequivalence of Amiodarone Hydrochloride Dispersible Tablets in human body. METHODS： By a 2-period randomized crossover design, 18 healthy male volunteers were assigned to receive oral single dose of Amiodarone Hydrochloride Dispersible Tablets （trial preparation） and Amiodarone Hydrochloride Tablets （reference preparation） . The plasma concentrations of amiodarone hydrochloride in 18 healthy male volunteers were determined by LC-MS; the pharmacokinetic parameters were calculated using, SPSS10.0 software and the bioequivalence of the two preparations of amiodarone hydrochloride was evaluated. RESULTS： The main pharmacokinetic parameters of Amiodarone Hydrochloride Dispersible Tablets （trial preparation） vs. Amiodarone Hydrochloride Tablets （reference preparation） were as follows： tmax （4.2± 1.2） b vs.（3.8±0.9） h; Cmax（420.0±211.7） ng · mL^-1 vs.（414.8± 166.7） ng · mL^-1, t1/2（38.8±20.4） h vs.（39.6± 12.5）h;AUC0-96（6 375.3±3 093.1）vs.（6 518.4 ±3 101.1）ng · h · mL^-1; AUC0-∞（7 165.3±3 680.2） ng · h· mL^-1 vs. （7 325.5 ± 3 478.1） ng · h· mL^-1 . The relative bioavailability of the test preparation of amiodarone hydrochloride was（98.4 ± 8.4）% as against the reference preparation of amiodarone hydrochloride. CONCLUSION： Amiodarone Hydrochloride Dispersible Tablets and Amiodarone Hydrochloride Tablets were bioequivalent.