四乙酰基葛根素自微乳化给药系统的制备及体外评价  

Preparation and in vitro evaluation of self-microemulsifying drug delivery system for tetra-acetylated puerarin

作　　者：谢欢[1] 周伟[1] 刘姹[1] 杨大坚[1] 

机构地区：[1]香港理工大学现代中药研究所暨深圳市中药药学及分子药理学研究重点实验室,广东深圳518057

出　　处：《中南药学》2010年第6期401-406,共6页Central South Pharmacy

基　　金：深港创新圈专项资助计划-应用研发专题(编号:SG200710190095A)

摘　　要：目的筛选四乙酰基葛根素自微乳化给药系统的处方并进行体外评价。方法测定四乙酰基葛根素在各种油相、表面活性剂和助表面活性剂中的溶解度,对不同溶剂进行初步配伍研究,采用三元相图法考察不同油相、表面活性剂和助表面活性剂形成微乳的能力,绘制不同处方组成的三元相图,以微乳外观、乳化速度、乳滴粒径、载药量为指标,进一步优选处方,找出最佳的组合和处方配比,制备自微乳化液,测定四乙酰基葛根素自微乳化制剂的溶出度。结果最佳处方体系为Labrafil M1944 cs-Polyoxy 35 castor oil-Transultol P(30∶40∶30)和LauroglycolFCC-Tween 80-Transcutol P(30∶30∶40),此处方体系能迅速乳化为外观澄清透明的微乳液,粒径分布为(21.6±5.1)、(20.2±9.8)nm,45 min内溶出度分别96.2%、96.7%。结论成功制备了四乙酰基葛根素自微乳化给药系统。Objective To prepare and evaluate the self-microemulsifying drug delivery system for tetra-acetylated puerarin.Methods The solubility of tetra-acetylated puerarin in various vehicles including oil,surfactant and cosurfactant was determined.The preliminary compatibility of various vehicles with high solubility of tetra-acetylated puerarin was studied.Ternary phase diagrams were constructed to identify the capability to form microemulsion of different oil,surfactants and cosurfactants.Appearance,self-emulsifying time,emulsion particle size,and amount of drug loading were used as the evaluation standard to optimize the formulations and determine the dissolution of the self-microemulsifying drug delivery system.Results The optimized formulations were Labrafil M 1944 cs-Polyoxy 35 castor oil-Transcutol P（30∶40∶30） and Lauroglycol FCC-Tween 80-Transcutol P（30∶30∶40） and could be emulsified into microemulsion with clear appearance and droplet size,and the distribution of two formulations were（21.6±5.1）and（20.2±9.8） nm.The dissolution of the two formulations in vitro at 45 min was 96.2% and 96.7%,respectively.Conclusion Self-micremulsifying drug delivery system for tetra-acetylated puerarin has been prepared.

关 键 词：四乙酰基葛根素 自微乳化给药系统 三元相图 

分 类 号：R943[医药卫生—药剂学] R927.2[医药卫生—药学]