【摘要】 目的探索卤泛群自微乳给药系统(halofantrine self-microemulsifying drug delivery system,HF-SMEDDS)通过改善淋巴转运增加HF口服生物利用度的可能性。方法以亚油酸乙酯为油相,吐温80为乳化剂,无水乙醇为助乳化剂,制备并筛选HF-SMEDDS处方,以油相和混合乳化剂(吐温80和无水乙醇)的比例及乳化剂与助乳化剂的比例为考察因素,以静脉给药组为对照,以二插管大鼠为动物模型,考察不同HF-SMEDDS处方口服给药后在大鼠体内的生物利用度。结果 9组处方HF-SMEDDS粒径分布在20.6～336.5 nm,经淋巴转运药量可达到总给药量的2.25%～19.6%。结论 HF-SMEDDS能有效提高药物的生物利用度,为HF口服制剂开发提供一定研究思路与基础。更多还原

【Abstract】 Objective To investigate the effect of halofantrine self-microemulsifying drug delivery systems(HFSMEDDS) on bioavailability improvement via enhancing the lymphatic transport after oral administration. Methods Using ethyl linoleate as the oil phase, Tween 80 as the surfactant and ethyl alcohol as the auxiliary surfactant, HFSMEDDS were prepared and the formulations were screened. With the proportion of oil phase to mixed emulsifier as well as the proportion of emulsifier to co-emulsifier as the factors, the bioavailability of different HF-SMEDDS formulations in rats were investigated by using intravenous administration group as the control and double cannulated rats as model animals. Results The average particle size of the nanoemulsions of different formulations was 20.6-336.5 nm and the translymphatic drug delivery reached 2.25 %-19.6 % of the total dose. Conclusion HF-SMEDDS can effectively improve the bioavailability of drugs and provide some research ideas and basis for the development of HF oral preparations.更多还原