Box-Behnken效应面法优化牛蒡苷pH敏感脂质体处方  

Optimization of pH-sensitive arctiin liposome precription by Box-Behnken response surface methodology

作　　者：武鑫朋[1] 孙李妍[1,2] 慕宏杰[1] 杨绍梅[1] 魏俊花[1] 周绣棣[1] 陈大全[1] 

机构地区：[1]烟台大学药学院,山东烟台264005 [2]烟台山医院,山东烟台264001

出　　处：《齐鲁药事》2011年第11期625-628,共4页qilu pharmaceutical affairs

摘　　要：目的以牛蒡苷(arctiin,AC)为模拟药,通过Box-Behnken效应面法优化制备AC-pH敏感脂质体。方法采用薄膜分散法制备脂质体,分别以磷脂-胆固醇比(X1)、磷脂-药质量比(X2)、pH敏感材料含量(X3)为考察对象,以包封率(Y1)、载药量(Y2)和粒径(Y3)为评价指标,利用三因素三水平Box-Behnken效应面设计法筛选牛蒡苷pH敏感脂质体的最佳处方;并考察该制剂的稳定性。结果牛蒡苷pH敏感脂质体的平均包封率为(93.25±1.5)%;平均载药量(94.10±1.8)%;平均粒径为(208.55±2.8)nm。室温下,AC脂质体为乳白色细腻乳液,对室温条件稳定,但对光照和60℃不稳定。结论采用Box-Behnken实验设计法优化牛蒡苷pH敏感脂质体处方可得到较高包封率、稳定性优良且pH敏感性良好的产品,并为今后进行体内剂型研究奠定基础。Objective To optimize and prepare pH - sensitive arctiin liposome by Box - Behnken response surface methodology. Methods The liposome was prepared by film dispersion method and optimized though a three factor and three - level Box - Behnken,with the lipid - cholesterol （ X1 ）, lipid - drug （ X2 ） and the content of pH - sensitive materials（X3 ） as the inde- pendent variables, and the entrapment efficiency （ Y1 ）, drug loading （ Y2 ）, particle diameter （ Y3 ） as the dependent variables. The stability of this praeparatum was investigated. Results The average entrapment efficiency, drug loading and particle diameter of pH - sensitive arctiin liposome were respectively （ 93.25 ± 1.5 ） %, （ 94.10 ± 1.8 ） % and （ 208.55 ± 2.8 ）nm. The arctiin li- posome was ivory polymeric emulsion and stable in room temperature, but instable to illumination and 60 ℃. Conclusion The high entrapment efficiency, stability and pH - sensitive product can be obtained by optimizing pH - sensitive arctiin liposome prescription with Box - Behnken experimental design method, and to provide a good foundation for dosage form study in vivo in the future.

关 键 词：牛蒡苷 pH敏感脂质体 薄膜分散法 Box—Behnken实验设计 

分 类 号：R944.9[医药卫生—药剂学]