论文部分内容阅读
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 and bioequivalence of dexlansoprazole sustained-release capsules in Beagle dogs. Methods The plasma concentration of dexlansoprazole dexamethasone sustained-release capsules and reference preparations of 10 Beagle dogs were determined by LC-MS / MS. The pharmacokinetic parameters were calculated. Results After a single oral administration of the test preparation and the reference preparation, the t1 / 2 of dexlansoprazole in plasma was (1.2 ± 1.0) and (1.0 ± 0.7) h respectively, and the tmax was (2.3 ± 1.0) and 2.6 ± 1.1 h and ρmax were (2.388 6 ± 0.639 1) and (2.348 5 ± 0.728 6) mg · L -1, respectively. The AUC0-t were (5.601 4 ± 1.627 4) and (5.602 3 ± 1.865 7) mg · h · L-1 and AUC0-∞ were 5.653 6 ± 1.630 9 and 5.657 5 ± 1.878 6 mg · h · L -1, respectively. The relative bioavailability of dexlansoprazole in the test formulation was (101.6 ± 8.9)% based on AUC0-t. After several oral administration of the main pharmacokinetic parameters and single oral basically the same. Conclusion The pharmacokinetic parameters of dexlansoprazole in Beagle dogs are quite different. The two formulations of dexlansoprazole sustained release capsules are bioequivalent.