4-氨基-2-三氟甲基苯基维甲酸酯自微乳胶囊的研制

Preparation of self-microemulsifying drug delivery systems containing 4-amino-2-trifluoromethyl-phenyl retinate

目的制备4-氨基-2-三氟甲基苯基维甲酸酯固体自乳化制剂,以解决该药水溶性差的问题,提高药物胃中溶出度和口服生物利用度。方法通过伪三元相图法考察不同乳化剂、助乳化剂和油相形成微乳的能力和区域,制备自微乳。然后采用mix-ture design方法进行处方优化,并对其乳化后粒径、制剂综合评分和载药量进行考察。结果制备出的最佳处方(含HS1570%,PEG400 10%,油酸乙酯20%)自乳化后粒径在30 nm左右,体外溶出10 min即可溶出80%以上。结论该处方制备出的ATPR固体自微乳可用于提高其溶出速度。

Objective Self-microemulsifying drug delivery system containing 4-amino-2-trifluoromethyl-phenyl retinate was prepared,in order to solve the problems of poor water solubility,to improve the solubility in the stomach and oral bioavailability.Methods Pseudoternary phase diagrams were used to evaluate the self-microemulsification existence area.Mixture design was used to optimize the formulation of ATPR self-microemulsifying.Particle size,drug loading and integrated evaluation were investigated.Results The optimal formulations（containing HS15 70%,PEG400 10%,Ethyl oleate 20%） had good self-microemulsifying efficiency.Particle size was about 30 nm and dissolution rate from solid ATPR SMEDDS was above 80% in 10 min.Conclusion The results indicated the potential use of SMEDDS for the delivery of 4-amino-2-trifluoromethyl-phenyl retinate to increase its dissolution rate.