盐酸曲马多缓释滴丸在比格犬体内的药动学

目的：研究盐酸曲马多（Tr）缓释滴丸在比格犬体内的药动学，评价其生物利用度。方法：6只Beagle犬雌雄各半，采用两制剂双周期随机交叉试验设计，分别单剂量口服Tr缓释滴丸和缓释片，用高效液相色谱-紫外（HPLC-UV）法测定曲马多的血药浓度。结果：Tr缓释滴丸和缓释片的C_max分别为（273.34±69.2）ng·mL^-1和（244.02±94.88）ng·mL^-1，T_max分别为（6.5±0.84）h和（6.0±0.89）h，AUC_0-t分别为（2 893.87±811.40）ng·h·mL^-1和（2 505.99±628.50）ng·h·mL^-1，试验制剂与参比制剂相对生物利用度为97.2%±13.6%，经统计学处理，试验制剂AUC_0-24的90%置信区间为96.4%~116.5%，C_max的90%置信区间为103.1%~114.9%。结论：Tr缓释滴丸和缓释片在体内的处置均符合一室模型，单次给药给予相同剂量时二者具有生物等效性。

Pharmacoknetic study of sustained release dropping pills of tramadol hydrochloride in Beagle dogs

OBJECTIVE To study the pharmacokinetics of sustained release dropping pills of tramadol hydrochloride in Beagle dogs and evaluate its bioavailability.METHODS 6 Beagle dogs with half males and half females were given a single oral dose of Tr sustained-release dripping pills and tablets, In a randomized cross-over manner, the concentration of tramadol was determined by HPLC-UV method.RESULTS The pharmacokinetics of tramadol sustained-release dripping pills and tablets were as follows:C_max (273.34±69.2) ng·mL^-1 vs. (244.02±94.88) ng·mL^-1, T_max (6.5±0.84) h vs. (6.0±0.89) h, AUC_0-t (2 893.87±811.40) ng·h·mL^-1 vs. (2 505.99±628.50) ng·h·mL^-1. The relative bioavailability of the test suppository was 97.2%±13.6% compared to reference suppository. The AUC_0-24 and C_max of the test suppository were within 96.4%-116.5% and 103.1%-114.9% of the test suppository using the 90% confidence interval.CONCLUSION The pharmacokinetic profile of Tr sustained-release dripping pills and tablets in Beagle dogs after single dose are both one-compartment model, Test suppository is bioequivalent to the reference suppository.