自微乳化给药系统促进卤泛群经淋巴转运的研究  

Study on Promotion of Lymphatic Transport of Halofantrine by Self-microemulsifying Drug Delivery Systems

作　　者：谭亚男 尹宗宁[2] TAN Ya-nan;YIN Zong-ning(Sichuan Institute of Food Inspection,Chengdu 611731,China;Key Laboratory of Drug Targeting and Drug Delivery System,Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu 610041,China)

机构地区：[1]四川省食品检验研究院,四川成都611731 [2]四川大学华西药学院靶向药物与释药系统教育部重点实验室,四川成都610041

出　　处：《食品与药品》2021年第4期332-337,共6页Food and Drug

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。Objective To investigate the effect of halofantrine self-microemulsifying drug delivery systems(HF-SMEDDS)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,HF-SMEDDS 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.

关 键 词：卤泛群 自微乳给药系统 二插管大鼠模型 淋巴转运 

分 类 号：R943[医药卫生—药剂学]