2种盐酸舍曲林制剂人体生物等效性研究

目的研究2种盐酸舍曲林制剂的人体生物等效性。方法采用双周期随机交叉设计试验,22名健康男性志愿者单剂量口服盐酸舍曲林口服液(受试制剂)或盐酸舍曲林片(参比制剂)50mg,以高效液相色谱-质谱联用法测定血药浓度。结果受试制剂与参比制剂的t1/2分别为(27.3±5.2)、(26.3±3.0)h,Cmax分别为(9.56±2.49)、(9.43±2.91)μg·L-1,tmax分别为(5.18±1.47)、(6.00±1.07)h,AUC0～108分别为(329±112)、(297±111)μg.h·L-1,AUC0～∞分别为(354±127)、(316±122)μg.h.L-1。经方差分析和双单侧t检验,主要药动学参数无差异,但tmax存在差异;受试制剂的相对生物利用度为(115.5±26.7)%。结论2种盐酸舍曲林制剂具有生物等效性。

Study on the Bioequiavailability of Two Sertralines Hydrochloride Formulations in Healthy Volunteers

OBJECTIVE:To study the bioequiavailability of two sertraline hydrochloride formulations in healthy volunteers.METHODS:A randomized, crossover study of 22 healthy volunteers receiving single oral dose of 50mg sertraline hydrochloride solution(test preparation) or sertraline hydrochloride tablets(comparator preparation) was conducted and the blood concentrations determined by LC/MS/MS.RESULTS: The pharmacokinetic parameters for the test sertraline and the comparator sertraline were as follows:t1/2 were (27.3±5.2)h and (26.3±3.0)h,respectively;Cmax were(9.56±2.49)μg·L-1 and(9.43±2.91)μg·L-1,respectively;tmax were(5.18±1.47)h and(6.00±1.07)h,respectively;AUC0～108 were(329±112)μg·h·L-1 and (297±111)μg·h·L-1,respectively;AUC0～∞ were(354±127)μg·h·L-1 and (316±122)μg·h·L-1,respectively.There were no significant differences in main pharmacokinetics parameters between the 2 preparations,except in tmax from analysis of variance and one-side & two-sides t tests.The relative bioavailability of the test sertraline was(115.5±26.7)%.CONCLUSION:These two sertraline hydrochloride formulations are bioequivalent.