多潘立酮自乳化软胶囊Beagle犬体内药物动力学研究

Pharmacokinetics of Domperidone Self-emulsified Soft Capsule in Beagle dogs

目的:对自制多潘立酮自乳化软胶囊进行Beagle犬体内药物动力学研究。方法:Beagle犬采用随机双交叉试验方法,对受试制剂(自制多潘立酮自乳化软胶囊)及参比制剂(法国杨森多潘立酮片剂)采用HPLC-MS法测定给药后不同时间的血药浓度,并用DAS 2. 0拟合药物动力学参数。结果:受试制剂:T_(1/2z)=89±12min,Cmax=59. 20±9. 66μg/L,Tmax=90±21min,AUC(0-∞)=11849. 71±1884. 22μg/(L·min)。参比制剂:T_(1/2z)=107±54min,Cmax=41. 80±8. 83μg/L,Tmax=120±21min,AUC(0-∞)=6376. 02±1341. 95μg/(L·min)。结论:多潘立酮软胶囊AUC曲线下面积明显高于法国杨森产品,其口服生物利用度有所提高。

Objective： To study the pharmacokinetics of domperidone self - emulsified soft capsule in beagle dogs. Methods： The Beagle dogs were randomized double - crossover test method and the plasma concentrations of the test preparations （ self - made domperidone self-emulsified soft capsules） and the reference preparations （the French poplar domperidone tablets） were determined by HPLC - MS at different times after administration. The DAS2.0 was used to fit the pharmacokinetic parameters. Results： Test preparation： T1/2x = 89 ± 12 min, Cmax =59.20 -＋9.66 μg/L,Tmax = 90 ± 21 min, AUC（0 -∞） = 11849.71 ± 1884.22 μg/（ L·min）. Referenee formulation： T1/2z = 107 ±54min, Cmax = 41.80 ± 8.83g/L, Tmax = 120 ± 21 min, AUC （0 - ∞ ） = 6376.02 ± 1341.95μg/ （L · min）. Conclusion： The area under the AUC curve of domperidone softgels is significantly higher than that of Freneh Yang Sen products, and its oral bioavailability is improved.