摘要
目的:采用星点设计-效应面法优化α-细辛脑脂质体喷鼻剂的制备工艺。方法:以乙醇注入法制备α-细辛脑脂质体喷鼻剂,采用星点设计-效应面法优化制备工艺,在单因素试验的基础上以磷脂含量、磷脂与胆固醇的质量比和磷脂与药物的质量比为自变量,以包封率为因变量,优化处方工艺,进行验证试验并在电镜下观察脂质体形态。结果:二项式方程拟合度高(R2=0.9074),预测性好;星点设计-效应面法优选出的最佳工艺条件为磷脂含量为4.5%、磷脂与胆固醇的质量比为7.5、磷脂与药物的质量比为45,测得包封率为68.1%;最佳工艺验证结果与二项式拟合方程预测值偏差为1.73%;制备的脂质体形态完整,双分子膜结构清晰,均属于单室脂质体。结论:应用星点设计-效应面法能够精确有效地优化α-细辛脑脂质体喷鼻剂的制备工艺,稳定可行。
OBJECTIVE： To optimize the preparation technology of α-Asarone liposome nasal spray by central composite de- sign-response surface methodology. METHODS： α-Asarone liposome nasal spray was prepared by ethanol injection method. A cen- tral composite design-response surface methodology was used to optimize the preparation technology. The formulation and technology were optimized by single factor test using the concentration of phospholipid, weight ratio of phospholipid to cholesterol and weight ratio of phospholipid to drug as independent variables, entrapment efficiency as dependent variable. The optimal technology was validated and the morphology of liposome was observed under electron microscope. RESULTS： The adjusted R2 （R2=0.907 4） value was high, indicating that the model was well adapted to the responses. The optimum technology was that phospholipid was 4.5%, weight ratio of phospholipid to cholesterol was 7.5, weight ratio of phospholipid to drug was 45 and entrapment efficiency was 68.1%. The deviation of results of optimal technology and predicted value of binominal fitted equation was 1.73 %. Prepared li- posome was complete in appearance with clear bimolecular film structure, all belonged to unilamelar liposome. CONCLUSIONS： Central composite design-response surface methodology is successfully used to optimize the preparation technology of a-Asarone li- posome nasal spray. The optimized technology is stable and feasible.
出处
《中国药房》
CAS
CSCD
2013年第5期431-434,共4页
China Pharmacy
基金
广东食品药品职业学院自然科学项目资助(No.2010YZ006)
关键词
Α-细辛脑
脂质体
喷鼻剂
制备
星点设计
效应面法
α-Asarone
Liposome
Nasal spray
Preparation
Central composite design
Response surface methodology
