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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 bioavailability of norcantharidin sustained-release pellets in rabbits. Methods: Twelve rabbits were randomly divided into two groups. The rats were given a single dose of 30 mg · kg -1 norcantharidin sustained-release pellet capsules (test preparation) and commercial norcantharidin tablets Preparation), blood samples were taken at different times, the blood concentration of rabbits was determined by HPLC and the pharmacokinetic parameters were calculated. Results: The Cmax of the reference preparation and the test preparation were (47.14 ± 9.67) and (31.28 ± 7.51) μg · ml -1, respectively, and the values of t max were 2.02 ± 0.65 and 6.09 ± 0.67) h; t 1/2 was (0.96 ± 0.61) and (2.82 ± 1.37) h respectively; AUC 0-24 h were 362.73 ± 34.27 and 416.21 ± 39.65 μg · h · ml respectively ~ (-1). CONCLUSIONS: There is a significant difference in the rate of absorption between the test and reference preparations, both of which are not bioequivalent.