曲普瑞林微球在beagle犬体内药动学及生物等效性研究  

A Study on the Pharmacokinetics and Bioequivalence of Triptorelin in Beagle Dogs

作　　者：龙镭 周长华[2] 王仁友 聂涛 陈健文[2] 

机构地区：[1]深圳翰宇药业股份有限公司,广东深圳518057 [2]中山大学药学院,广东广州510006

出　　处：《湖北民族学院学报（医学版）》2011年第2期32-33,36,共3页Journal of Hubei Minzu University(Medical Edition)

摘　　要：目的研究醋酸曲普瑞林微球在beagle犬体内的药代动力学及生物等效性。方法 12条健康雄性beagle犬随机分成2组,100μg/kg单剂量肌注受试或参比醋酸曲普瑞林微球,放射免疫法测定beagle犬血清中睾酮的浓度,计算药动学参数和相对生物利用度。结果受试和参比醋酸曲普瑞林微球主要药动学参数AUC0-42d分别为:(90 252.01±3 109.51)与(92 536.17±3 387.27)ng/dL.h,Cm ax为(679.89±80.01)与(727.31±211.76)ng/dL,Tm ax为(3.91±0.65)与(4.05±0.51)h,受试曲普瑞林的相对生物利用度为(95.47±11.02)%。结论两种醋酸曲普瑞林微球的药动学过程基本一致,具有生物等效性。Objective To study the pharmacokinetics and bioequivalence of triptorelin acetate microsphere in the beagle dogs.Methods 12 healthy beagle dogs were randomly divided into two groups（test and reference groups）.A single dose of triptorelin acetate microsphere（100 μg/kg of test or reference preparation） was administered to beagle dogs by intramuscular injection.The concentration of testosterone in serum was determined by RIA.Then the main pharmacokinetic parameters and the relative bioavailability were analyzed.Results The main pharmacokinetic parameters of test and reference preparation were as follows：AUC0-42d（90 252.01±3 109.51） and（92 536.17±3 387.27） ng/dL·h,Cmax（679.89±80.01） and（727.31±211.76）ng/dL,Tmax（3.91±0.65） and（4.05±0.51）h,respectively.The relative bioavailability of the test preparation was（95.47±11.02）%.Conclusion The results of statistical analysis showed that the pharmacokinetics of two preparations were the same,and the two preparations were bioequivalent.

关 键 词：曲普瑞林 药动学 生物等效性 睾酮 放射免疫 

分 类 号：R969.1[医药卫生—药理学] R977.1[医药卫生—药学]