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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Cmax分别为(273.34±69.2)ng·mL-1和(244.02±94.88)ng·mL-1,Tmax分别为(6.5±0.84)h和(6.0±0.89)h,AUC0-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AUC0-24的90%置信区间为96.4%~116.5%,Cmax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。
Objective: To study the pharmacokinetics of tramadol hydrochloride (Tr) sustained-release dropping pills in beagle dogs and evaluate its bioavailability. Methods: Six Beagle dogs were randomly divided into two groups. The two-dose randomized crossover trial was designed. Single-dose oral sustained-release dropping pills and extended release tablets were prepared. The content of tramadol was determined by high performance liquid chromatography-ultraviolet Blood concentration. Results: The C max of sustained release dropping pills and sustained release tablets were (273.34 ± 69.2) ng · mL -1 and (244.02 ± 94.88) ng · mL -1, respectively, and the T max were (6.5 ± 0.84) h and (6.0 ± 0.89 ) h and AUC0-t were (2 893.87 ± 811.40) ng · h · mL-1 and (2 505.99 ± 628.50) ng · h · mL-1, respectively. The relative bioavailability of test and reference preparations was 97.2% ± 13.6% .Through statistical analysis, the 90% confidence interval of test preparation AUC0-24 was 96.4% ~ 116.5% and the 90% confidence interval of Cmax was 103.1% ~ 114.9%. Conclusion: The sustained-release dropping pills and sustained-release tablets of Tr both meet the one-compartment model and are bioequivalent when the same dose is administered in a single dose.