酮基布洛芬单室渗透泵片在家犬体内的药动学和相对生物利用度

The bioavilability and pharmacokinetics study of ketoprofen monolithic osmotic pump controlled-release tablets in dogs

目的:研究家犬口服酮基布洛芬单室渗透泵片的药动学和相对生物利用度。方法:家犬6只采用双周期交叉给药,用高效液相色谱法测定酮基布洛芬的血药浓度,用3P97处理药动学参数进而计算相对生物学利用度。结果:酮基布洛芬单室渗透泵片和市售普通片在家犬体内过程均符合单室模型,其主要的药动学参数Tmax,Cmax和AUC0-t分别是(2.51±0.67),(1.44±0.26)h;(7.12±1.27),(6.01±1.65)mg.L-1;(66.15±2.32),(59.28±3.69)μg.h.mL-1。结论:酮基布洛芬单室渗透泵片具有明显的缓释特征,生物利用度与市售普通片等效。

OBJECTIVE To study the pharmacokinetics and relative bioavilability of ketoprofen in dogs. METHODS Six dogs were divided into two groups by double crossing method in two weeks, The ketoprofen in plasma was measured by HPLC. The relative bioavilability and pharmacokinetic parameters of ketoprofen monolithic osmotic pump controlled-release tablets were computed by 3P97. RESULTS The pharmacokinetic parameters of test and reference preparation for ketoprofen were= Tmax （2. 51 ± 0. 67）and（1.44± 0. 26）h, Cmax （7. 12 ± 1. 27）and（6. 01 ± 1.65）mg·L^-1, AUC0-t （66. 15 ± 2. 32）, （59, 28 ± 3. 69）μg·h·mL^-1 ,respectively. The relative bioavilability of the controlled-release tablets was 110, 58%. CONCLUSION Ketoprofen monolithic osmotic pump controlled-release tablets have marked controlled-release characters. The ketoprofen monolithic osmotic pump controlled-release tablets and the normal tablets were bioequivalent.