摘要
目的确定双嘧达莫(DIP)肺靶向脂质体的较优处方。方法以薄膜蒸发法制备DIP肺靶向脂质体,采用星点设计-效应面法优化处方,以药/磷脂(%)、胆固醇/磷脂(%)和DIP投药量(mg)为自变量,包封率(%)、收率(%)、粒径(μm)与5μm的差值和径距为因变量,计算总评归一值,分别进行多元线性和非线性拟合,用效应面法预测较佳处方。结果总评归一值的多元非线性拟合方程优于多元线性回归方程,根据效应面得到较佳处方范围。以优化处方制备样品,各指标实测值与预测值偏差较小。结论星点设计-效应面法可以准确快速地优化DIP肺靶向脂质体的处方。
OBJECTIVE To determine the optimal formulation of pulmonary targeting dipyridamole （DIP） liposomes. METHODS The liposomes were prepared by film-evaporated technique. The formulation was optimized using central composite design and response surface methodology. The effects of three independence variables, DIP/phosphatidylcholine （ % ）, cholesterol/phosphatidylcholine （ % ） and DIP content （mg）, were evaluated. Response variables selected in the research were entrapment efficiency （ % ）, yield （ % ）, 5-particle size （μm） and span. The data were transformed into desirabilities. Overall desirability was calculated from the geometric mean of the four desirabilities of each formulation. The second-order polynomial and linear equations were fitted to the data of overall desirabilities, and the resulting equation was used to produce 3-D response surface graphs, through which optimal formulation were predicted. RESULTS The second-order polynomial equation was superior to the linear one. An optimal formulation was prepared according to the optimal experimental conditions and evaluated for entrapment efficiency, yield, particle size and span. The observed values agreed well with model predicted values. CONCLUSION Central composite design-response surface methodology is successfully used to optimize the formulation of pulmonary targeting DIP liposomes.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第10期762-765,共4页
Chinese Pharmaceutical Journal
关键词
双嘧达莫
肺靶向脂质体
星点设计-效应面法
归一值
dipyridamole
pulmonary targeting liposomes
central composite design-response surface methodology
desirability
