去甲斑蝥素缓释微丸胶囊家兔体内生物利用度研究

Study on Bioavailability of Norcantharidin Sustained Release Pellets Capsules in Rabbits

目的:研究去甲斑蝥素缓释微丸胶囊在家兔体内的生物利用度。方法:将12只家兔随机分成2组,分别单剂量灌服30mg·kg^(-1)去甲斑蝥素缓释微丸胶囊(受试制剂)和市售去甲斑蝥素片(参比制剂),不同时间采集血样,采用HPLC法测定家兔体内的血药浓度并计算药动学参数。结果:参比制剂与受试制剂的C_(max)分别为(47.14±9.67)、(31.28±7.51)μg·ml^(-1);t_(max)分别为(2.02±0.65)、(6.09±0.67)h;t_(1/2)分别为(0.96±0.61)、(2.82±1.37)h;AUC_(0～24h)分别为(362.73±34.27)、(416.21±39.65)μg·h·ml^(-1)。结论:受试制剂与参比制剂的吸收速率有显著差异,两者不具有生物等效性。

Objective： To study the pharmacokinetics and bioequivalence of norcantharidin sustained release pellets capsules in healthy rabbits. Method： Twelve rabbits were randomly divided into two groups, received oral single dose of norcantharidin sustained release pellets capsules 30 mg（test capsules）or noreantharidin tablets from market （reference tablets）. Plasma samples were collected at different time points. Plasma concentration of norcantharidin was determined by HPLC and pharmacokinetic parameters were calculat- ed. Result： The pharmaeokinetic parameters of reference tablets and test capsules were as the follows： Cmax of （47. 14 ± 9. 67） and （31.28±7.51） μg·ml^-1,tmaxof（2.02 ±0.65） and （6. 09 ±0.67） h,t1/2of（0.96± 0.61） and （2. 82 ± 1.37） h,AUC0-24hof （362. 73 ± 34. 27 ） and （416. 21 ± 39. 65 ） μg· h· ml^-1. Conclusion： The absorption rate of test capsules is different from reference tablets. The capsules and the tablets of noreantharidin are not bioequivalent.