盐酸曲马多缓释滴丸在比格犬体内的药动学  

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

作　　者：智成芳 曲韵智 王金 景舒 李津明[4] 

机构地区：[1]内蒙古科技大学包头医学院第二附属医院药剂科,内蒙古包头014030 [2]北京正大绿洲医药科技有限公司,北京101113 [3]内蒙古医科大学药学院药剂教研室,内蒙古呼和浩特010110 [4]哈尔滨商业大学药学院,黑龙江哈尔滨150076

出　　处：《中国医院药学杂志》2017年第22期2236-2238,2242,共4页Chinese Journal of Hospital Pharmacy

基　　金：内蒙古自治区自然科学基金项目(编号:20080404MS1206)

摘　　要：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 sustained release dropping pills of tramadol hydrochloride in Bea- gle 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.. Cmax （273. 34± 69. 2） rig-mL-1 vs. （244. 02± 94. 88） ng. mL l, Tmax （6. 5± 0. 84） h vs. （6. 0 ± 0. 89） h, AU0-t （2 $93. 87 ± 811.40） ng. h, mL 1 vs. （2 505.99 ± 628. 50） rig. h·mL^- 1. The relative bioavailability of the test supposi- tory was 97. 2%± 13. 6% compared to reference suppository. The AUCo24 and Cmax 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 pharmacoki- netic 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.

关 键 词：盐酸曲马多 药动学 相对生物利用度 生物等效性 

分 类 号：R965[医药卫生—药理学]