氟比洛芬微乳大鼠药动学研究

Pharmacokinetics of Flurbiprofen Microemulsion in Rats

目的评价自制氟比洛芬微乳在大鼠体内的药动学和相对生物利用度。方法两组SD雄性大鼠分别单剂量给予氟比洛芬微乳和氟比洛芬片,采用HPLC测定血药浓度。应用3P87药动学程序对数据进行处理计算药动学参数。结果单剂量给药后氟比洛芬微乳和氟比洛芬片的主要药动学参数Cmax分别为(4976.1±500.9)ng·mL-1和(3684.0±500.6)ng·mL-1,tmax分别为(1.17±0.37)h和(2.33±0.46)h,AUC0→36分别为(44613.5±8515.7)ng·mL-1和(34126.5±7909.6)ng·h·mL-1,相对生物利用度为130.46%。结论以市售氟比洛芬片为参比制剂,氟比洛芬微乳在大鼠体内的生物利用度明显提高。

OBJECTIVE To study the pharmacokinetics and relative bioavailability of flurbiprofen microemulsion in rats. METHODS Single dose po flurbiprofen microemulsion and tablet were given to two groups of rats respectively. The plasma concentration of flurbiprofen was determined by ttPLC and the data was processed with the software 3P87. RESULTS The C t A UC0→36 of flurbiprofen microemulsion and flurbiprofen tablet were （4 976.1± 500.9） ng·mL ^-1 and （3 684.0 ± 500.6） ng·mL^-1, （1.17 ±0.37）h and （2.33 ±0.46）h,（44 613.5±8 515.7） ng·h·mL^-1 and （34 126.5 ±7 909.6）ng ·h·mL^-1 ,respectively. The mean relative bioavailability of the flurbiprofen microemulsion was 130.46%. CONCLUSION The results suggested that the flurbiprofen microemulsion has improved the bioavailability in rats.