自制甲硝唑缓释微球结肠溶胶囊在家兔体内药代动力学研究

Study on the pharmacokinetics of colonic-coated capsules containing metronidazole-loaded sustained release microspheres in rabbits

目的研究甲硝唑缓释微球结肠溶胶囊在家兔体内的药代动力学,评价其在结肠的释放及吸收特性。方法选取家兔作为受试动物,双周期交叉设计,采用高效液相色谱法测定家兔静脉血中的甲硝唑浓度,计算药代动力学参数。结果实验组:ke0.259/h,t1/22.679h,Tmax8.5h,Cmax4.617μg/ml,AUC25.279μg·h/ml;对照组:ke0.325/h,t1/22.133h,Tmax1h,Cmax13.499μg/ml,AUC49.889μg·h/ml;实验组相对生物利用度为50.7%。结论甲硝唑微球结肠溶胶囊在结肠内缓慢释放,降低了血药浓度。

Objective To investigate the pharmacokinetics of colonic-coated capsules containing metronidazole-loaded sustained-release microspheres in rabbits, and to evaluate the characteristics of release and absorption in colon. Methods The rabbits were used as animal models and two-cycle crossover design was used. The metronidazole concentration in venous blood of rabbits was determined by high performance liquid chromatography and the parameters of pharmaeokinetics were calculated. Results In experiment group： ke 0. 259/h, tl/2 2. 679h,Tmax 8.5 h, Cmax 4. 617μg/ml, AUC 25. 279μg · h/ml. However in control group： ke 0. 325/h, tl/2 2. 133h ,Tmax 1 h, Cmax 13. 499 μg/ml, AUC 49. 889 μg · h/ml. The relative bioavailability in experiment group was 50. 7%. Conclusion The release of colonic-coated capsules containing metronidazole-loaded sustainedrelease microspheres in colon is sustained, as a result, the metronidazole concentration in blood is lowered.