氯雷他定口腔崩解片人体生物等效性研究

 目的对国产氯雷他定口腔崩解片和进口普通片进行生物等效性研究。方法20名健康男性志愿者按2×2交叉试验方案设计,分别口服受试制剂和参比制剂各20mg,并采集36h内动态血标本;采用HPLC/MS测定血浆中氯雷他定浓度,计算药动学参数,并判定两种制剂是否生物等效。结果受试制剂和参比制剂的主要药动学参数ρ_max分别为(19.57±11.09)和(18.97±10.76)μg·L^-1,t_max分别为(0.8±0.2)和(0.8±0.2)h,AUC_0-36分别为(44.9±17.6)和(42.9±14.6)μg·h·L^-1,AUC_0-∞分别为(52.6±24.2)和(50.2±19.6)μg·h·L^-1,t_1/2(ke)分别为(13.1±6.3)和(13.9±6.8)h,两制剂主要药动学参数经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂的人体生物利用度为(103.2±9.0)%。结论两种制剂生物等效。

Study on Bioequivalence of Loratadine Orally Disintegrating Tablets in Chinese Healthy Volunteers

OBJECTIVE To study the bioequivalence of loratadine orally disintegrating tablets in Chinese healthy volunteers.METHODS Test preparation(20 mg) and reference preparation(20 mg) were given to 20 male healthy volunteers in randomized two-way crossover design for the pharmacokinetic and relative bioavailability study.Plasma concentrations of loratadine were determined by HPLC/MS.RESULTS The main pharmacokinetic parameters of the two preparations were as follows:ρ_max (19.57±11.09) and(18.97±10.76)μg·L^-1 ,t_max (0.8±0.2) and (0.8±0.2)h,AUC_0-36 (44.9±17.6) and (42.9±14.6)μg·h·L^-1 ,AUC_0-∞(52.6±24.2) and (50.2±19.6)μg·h·L^-1,t_1/2(ke) (13.1±6.3)and (13.9±6.8)h,respectively.The mean relative bioavailability of test preparation vs reference preparation were (103.2±9.0)%.CONCLUSION The statistical analysis shows the two preparations are bioequivalent.