醋酸艾司利卡西平片在比格犬体内的相对生物利用度

The relative bioavailability of eslicarbazepine acetate tablets in Beagle dogs

采用单剂量随机交叉实验设计,评价8只比格犬口服受试或参比醋酸艾司利卡西平片的相对生物利用度。用UPLC-MS/MS法测定血浆中的艾司利卡西林浓度,艾司利卡西平的线性范围为：1.0～1000.0ng/ml;定量下限可达1.0ng/ml;受试和参比制剂的主要药动学参数分别为：T_（max）（1.72±1.2）和（1.50±0.9）h;C_（max）（31300±14104）和（40088±18156）ng/ml,AUC_（0-t）（133121±60209）和（146 926±61 557）ng·h/ml,AUC_（0-∞）（133 171±60 207）和（147 028±615 93）ng·h/ml,t_（1/2）（5.84±2.0）和（5.80±1.1）h。受试制剂艾司利卡西平的相对生物利用度为（106.1±102.6）%。结果显示：两制剂平均药动学参数无统计学差异。

The relative bioavailability of eslicarbazepine acetate tablets in eight Beagle dogs was evaluated by a randomized single-dose cross-over design.The concentration of eslicarbazepine in plasma was determined by UPLC-MS/MS.The calibration curve for eslicarbazepine was linear in the range of 1.0～1 000.0 ng/ml with the lower limit of quantification 1.0ng/ml.The main pharmacokinetic parameters for test and reference preparations were as follows：T_（max）（1.72±1.2） and（1.50±0.9）h;C_（max）（31 300±14 104） and（40 088±18 156） ng/ml,AUC_（0-t）（133 121±60 209） and（146 926±61 557） ng·h/ml,AUC_（0-∞）（133 171±60 207） and（147 028±61593） ng-h/ml,t_（1/2）（5.84±2.0） and（5.80±1.1） h.The relative bioavailability of eslicarbazepine acetate tablets for test preparations was（106.1±102.6）%.The results showed that these two preparations had no significant difference in the average pharmacokinetic parameters.