摘要
目的采用星点设计-效应面法优化依西美坦自微乳化给药系统。方法选择了适宜的油、表面活性剂和助表面活性剂,即以Maisine 35-1-Neboee-M5(1∶1)作为油相,Cremopher EL-Labrasol(4∶1)为乳化剂,Transcutol P作为助乳化剂。乳化剂与助乳化剂的比例Km和含油量作为考察因素,以微乳粒径、Zeta电位、药物平衡溶解度、昙点、5和60 min时药物的累积溶出量作为效应值,应用Design Expert进行处方优化,并对优化处方进行验证。结果通过星点效应面优化快速获得依西美坦自微乳的优化处方组成范围,如油相-表面活性剂-助表面活性剂(31∶49∶20)。结论通过星点设计-效应面法适用于依西美坦自微乳化给药系统的处方优化,所建立的数学模型预测性良好。
OBJECTIVE To optimize the formulation of exemestane self-microemulsions drug delivery system using central composite design-response surface methodology.METHODS The system was optimized using Design Expert software.Particle size,Zeta potential,solubility,cloud point and the cumulative dissolution percentage of exemestane at 5 min and 60 min were taken as dependentvariables,and the usage amount of oil and Km as the independent variables.RESULTS The optimized formulation was quickly and conveniently obtained by the central composite design-response surface methodology,i.e.oil-surfactants-cosurfactants（31∶49∶20）.CONCLUSION The central composite design and response surface methodology is useful for the formula optimization of exemestane self-microemulsions drug delivery system.The prediction accuracy of the established model is good.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2011年第7期532-536,共5页
Chinese Pharmaceutical Journal
关键词
依西美坦
自微乳
星点设计
效应面法
exemestane
self-microemulsions
central composite design
response surface methodology
