星点设计效应面法优化非洛地平自微乳给药系统

目的 设计非洛地平自微乳给药系统，并进行体外评价。方法 测定非洛地平的溶解度，考察油相与乳化剂的相容性，绘制伪三元相图，初步设计自微乳处方；运用星点设计效应面法优化自微乳处方；评价自乳化性能和体外溶出行为。结果 非洛地平自微乳处方：油相LABRAFIL M 1944CS为4.4 g，乳化剂Cremophor EL35为5.5 g，助乳化剂PEG400为1.1 g，非洛地平1.0 g；自乳化效率高，乳液澄明稳定，平均粒径为30.4 nm，PDI为0.16；水中溶出很快，5 min内平均溶出度>85%，30 min达99%，24 h后乳滴依然稳定。结论 星点设计-效应面法优化的非洛地平自微乳，自乳化性能高，乳液稳定，显著提高非洛地平的体外溶出度。

Optimization of Felodipine Self-microemulsifying Drug Delivery System by Central Composite Design-response Surface Methodology

OBJECTIVE To optimize and assess the formulation of self-microemulsifying drug delivery system mixture for felodipine. METHODS By the means of solubility, compatibility, ternary phase diagram and central composite design-response surface methodology, the preliminary formulation was settled. The self-microemulsifying efficiency, stability and dissolution were studied. RESULTS The optimized formulation was composed of LABRAFIL M 1944CS 4.4 g, Cremophor EL35 as a emulsifier 5.5 g, PEG400 1.1 g, and felodipine 1.0 g. The average particle size after the emulsification was 30.4 nm, and PDI was 0.16. The self-emulsifying efficiency and stability was excellent, and accumulative dissolution reached 85% in 5 min, and 99% in 30 min. After 24 h, the felodipine self-microemulsifying particles was still stable. CONCLUSION By the means of central composite design-response surface methodology, a felodipine self-microemulsifying mixture was obtained, which showed a high self-emusifying efficiency, stability and a good in vitro dissolution performance.