右旋兰索拉唑缓释胶囊在Beagle犬体内的药动学及生物等效性  

Pharmacokinetics and bioequivalence of dexlansoprazole delayed release capsules in Beagle dogs

作　　者：孟庆彬[1] 唐静雅[1] 周立华[1] 周艺佳 侯媛媛[1] 孙璐[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2015年第5期370-375,399,共7页Journal of Shenyang Pharmaceutical University

摘　　要：目的研究右旋兰索拉唑缓释胶囊在Beagle犬体内的药动学特征及生物等效性。方法采用LC-MS/MS法测定10只Beagle犬单次和多次口服右旋兰索拉唑缓释胶囊受试制剂和参比制剂后的血药质量浓度,计算药动学参数。结果单次口服受试制剂和参比制剂后,血浆中右旋兰索拉唑的t1/2分别为(1.2±1.0)和(1.0±0.7)h,tmax分别为(2.3±1.0)和(2.6±1.1)h,ρmax分别为(2.388 6±0.639 1)和(2.348 5±0.728 6)mg·L-1,AUC0-t分别为(5.601 4±1.627 4)和(5.602 3±1.865 7)mg·h·L-1,AUC0-∞分别为(5.653 6±1.630 9)和(5.657 5±1.878 6)mg·h·L-1。以AUC0-t计算,受试制剂中右旋兰索拉唑的相对生物利用度为(101.6±8.9)%。多次口服给药后的主要药动学参数与单次口服基本一致。结论右旋兰索拉唑的药动学参数在Beagle犬体内个体差异较大,右旋兰索拉唑缓释胶囊的两种制剂生物等效。Objective To study the pharmacokinetics profile of dexlansoprazole delayed release capsules in beagle dogs.Methods Ten Beagle dogs were administered with an oral single and multiple doses of test and reference capsules of dexlansoprazole in a randomized two-way cross-over test and the plasma concentrations of dexlansoprazole were determined by LC-MS/MS method.The pharmacokinetic parameters were calculated by Win Nolin 6.1 software.Results The main pharmacokinetic parameters of dexlansoprazole test and reference capsules after a single dose were as follows： t1 /2=（1.2 ± 1.0） and（1.0 ± 0.7） h; tmax=（2.3 ± 1.0）and（2.6 ± 1.1） h; ρmax=（2.388 6 ± 0.639 1） and（2.348 5 ± 0.728 6）mg·L^-1; AUC0-t=（5.601 4 ±1.627 4） and（5.602 3 ± 1.865 7）mg·h·L^-1; AUC0-∞=（5.653 6 ± 1.630 9） and（5.657 5 ± 1.878 6）mg·h·L^-1,respectively.The relative bioavailability was（101.6 ± 8.9） %.The main pharmacokinetic parameters after multiple doses were similar to those after a single dose.Conclusions There is a significant individual difference on dexlansoprazole in Beagle dogs.The two kinds of dexlansoprazole delayed release capsules are bioequivalent in Beagle dogs.

关 键 词：右旋兰索拉唑 药动学 生物等效性 

分 类 号：R917[医药卫生—药物分析学]