双氯芬酸赖氨酸盐缓释片家犬体内药物动力学研究

Pharmacokinetics study of Diclofenac lysine sustained-release tablet in dogs

目的 以双氯芬酸钠缓释片为参比制剂 ,测定自制双氯芬酸赖氨酸盐缓释片家犬体内药物动力学参数。方法 选择3只家犬 ,用自身交叉对照实验方法 ,分别单剂量灌服双氯芬酸钠缓释片 ,自制双氯芬酸赖氨酸盐缓释片各 2片 ,由HPLC法测定药物浓度 ,紫外检测。结果 各方法的线性良好 ,加样回收率均在 90 %～ 10 5 %之间 ,日内日间精密度均小于 10 %。双氯芬酸钠缓释片 ,自制双氯芬酸赖氨酸盐缓释片中双氯芬酸钠Tmax 分别为 4h和 4 .5h ,Cmax 为 4 .0 6 2、4 .5 35mg·L-1;AUC0 -∞ 分别为38.2 2、4 2 .33mg·h·L-1相对生物利用度 10 1.3%。结论 两种制剂生物利用度无显著性差异。

Aim To investigate pharmacokinetics of diclofenac sodium(DS) between the two tablets diclofenac sodium sustained-release tablet and Diclofenac acid lysine(DAL) sustained-release tablet,a single oral dose study with 3 dogs was conducted according to crossover design.Methods The samples in plasma were assayed by HPLC methods with ultraviolet detection which used a C 18 column at 278nm.Results These methods exhibited large linear range with recovery ranged from 90% to 105%,intra-day and inter-day precision and accuracy were less than 10%.The pharmacokinetics parameters for DAL of two tablets were:T max 4h and 4.5h;C max 4.062 and 4.535mg·L -1 ;AUC 0-∞ 38.22 and 42.33mg·h·L -1 ,respectively.The relative bioavailability was 101.3%.Conclusion The bioavailability of the two tablets had no significant difference.