响应面法优化龙胆苦苷脂质体的复乳法制备工艺  

Optimization of the multiple emulsion formulation of gentiopicroside liposome using response surface methodology

作　　者：姚新武[1] 刘长霞[1] 张鹏[1] 

机构地区：[1]北京化工大学生命科学与技术学院,北京100029

出　　处：《北京化工大学学报（自然科学版）》2012年第2期68-73,共6页Journal of Beijing University of Chemical Technology(Natural Science Edition)

摘　　要：采用复乳法制备脂质体,使用3因素3水平的Box-Behnken响应面设计,以脂质体的包封率、载药量和综合评价为响应值,考察龙胆苦苷药液质量浓度、第一次乳化超声时间及膜材中磷脂与胆固醇的质量比对响应值的影响,并用Design-Expert 7.1.3软件(试用版)进行数据拟合、数学建模和预测分析。优化出的龙胆苦苷脂质体的最佳处方为龙胆苦苷药液质量浓度为2.04 mg/mL、第一次乳化超声时间为7.07 min、脂质体膜材中胆固醇与磷脂质量比为0.45。研究结果表明,在最优处方下龙胆苦苷脂质体形态完整、状态稳定,平均粒径为131 nm,其包封率为52.39%,与预测值的偏差率小于1%。A liposome was prepared by a multiple emulsion method which was guided by a three-factor, three-level Box-Behnken design. The design factors were the concentration of gentiopicroside （X1 ） , the time of ultrasound treatment during the first emulsification （X2 ）, and the cholesterol to egg yolk phosphatidylcholine （EPC） mass ratio （ X3 ） , and the response values were entrapment efficiency （ Y1 ） , drug loading capacity （ Y2 ） , and the comprehensive evaluation （Y3）. The data fitting, mathematical modeling and predictive analysis were carried out using Design Expert 7. 1.3 （Beta Edition）. The optimized formulation was as follows ： X1, X2 and X3 levels of 2.04 mg/ mL, 7.07 min, and 0.45, respectively. The results of the study showed that under the optimized formulation conditions, the liposome had a complete shape and steady state, and the diameter was 131 nm, and the entrapment efficiency was 52.39% , which differed from the predicted values by less than 1%.

关 键 词：响应面法 龙胆苦苷 脂质体 复乳法 处方优化 

分 类 号：R945[医药卫生—微生物与生化药学]