地洛他定胶囊人体药动学和生物等效性评价  

Study on the pharmacokinetics and bioequivalence of desloratadine capsules and reference tablets in healthy volunteers

作　　者：谌叶香 邹健军[2] 龚厚军[1] 李妩真 杨泽英[1] 肖大伟[2] 

机构地区：[1]湖南省怀化市第二人民医院,湖南怀化418200 [2]南京医科大学附属南京第一医院国家药物临床研究基地,江苏南京210006

出　　处：《中国现代应用药学》2005年第z2期736-738,共3页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的研究地洛他定胶囊和地洛他定片在人体的药动学和生物等效性。方法 20名健康受试者随机交叉单剂量口服地洛他定胶囊或地洛他定片20 mg后,采用高效液相色谱-质谱联用(HPLC-MS)测定血浆中地洛他定的经时血药浓度,计算其药动学参数和相对生物利用度,评价两种制剂的生物等效性。结果经3P97拟合,两者的体内过程皆符合口服给药一室模型,采用梯形法计算的两者AUC_(0-72)分别为(238.22±57.18)μg·h·L^(-1)和(247.66±73.34)μg·h·L^(-1),C_(max)均值分别为(13.70±4.27)μg·L^(-1)和(14.31±4.53)μg·L^(-1),t_(max)均值分别为(2.2±0.7)h和(2.3±0.9)h,地洛他定胶囊对地洛他定参比片的相对生物利用度为(96.4±6.3)%。结论两种制剂具有生物等效性。OBJECTIVE To study the pharmacokinetics and bioequivalence of desloratadine capsules and reference tablets in healthy volunteers.METHODS A single oral dose of 20 mg desloratadine capsules and reference tablets were given to 20 healthy male volunteers in an open randomized crossover design.Desloratadine concentrations in plasma were determined by HPLC-MS.The pharmacokinetic parameters and relative bioavailability were calculated by 3P97 program to evaluate the bioequivalence of the two preparations.RESULTS The concentration time curves of the two preparations are fitted to one-compartment model.Their main pharmacokinetic parameters were as follow:AUC_(0-72)were(238.22±57.18)g·h·L^(-1)and(247.66±73.34) ug·h·L^(-1),C_(max) were(13.70±4.27)μg·L^(-1)and(14.31±4.53)μg·L^(-1),and tmax were(2.2±0.7)hand(2.3±0.9)h,respectively.The relative bioavailability of desloratadine capsules to reference tablets was(96.4±6.3)%.CONCLUSION The statistical analysis of the result shows that the two preparations were bioequivalent.

关 键 词：地洛他定 高效液相色谱-质谱联用 药物动力学 生物等效性 

分 类 号：R976[医药卫生—药品]