正交设计优化磷酸川芎嗪-冰片脂质体的制备工艺  

Optimization of the Preparation Technology of Tetramethylpyrazine Phosphate-Borneol Liposome by Orthogonal Design

作　　者：刘剑敏[1] 唐静宜[1] 程路 陈凡[1] LIU Jianmin;TANG Jingyi;CHENG Lu;CHEN Fan(Department of Pharmacy,Wuhan NO.1 Hospital,Wuhan,Hubei,China 430022)

机构地区：[1]湖北省武汉市第一医院药学部

出　　处：《中国药业》2019年第11期44-47,共4页China Pharmaceuticals

基　　金：湖北省武汉市卫生计生委科研项目[WZ16D06];北京医卫健康公益基金会医学科学研究基金[YWJKJJHKYJJ-B17708];湖北省卫生计生委面上科研项目[WJ2017M180]

摘　　要：目的优化磷酸川芎嗪(TMPP)-冰片(B)脂质体的制备方法。方法采用乙醇注入式(NH4)2SO4梯度法制备TMPP-B脂质体,利用超速离心法测定包封率。以包封率为考察指标,通过正交设计考察磷脂-胆固醇质量比(因素A)、TMPP-(磷脂+胆固醇)质量比(因素B)、水化时间(因素C)和(NH4)2SO4浓度(因素D)对制备工艺的影响。结果对TMPP-B脂质体包封率的影响顺序为A>D>B>C,最佳工艺条件为A1B2C1D2。按此优化工艺制备3批TMPP-B脂质体,其平均粒径为(136.10±6.30)nm,分布均匀,Zeta电位为(-35.70±3.60)mV,TMPP包封率为(73.14±0.71)%。结论该制备工艺的脂质体包封率高,分布均匀,形态好,质量稳定,该方法简单合理。Objective To optimize the preparation technology of tetramethylpyrazine phosphate(TMPP)-borneol(B)liposome.Methods The TMPP-B liposomes were prepared by the ethanol injection method combined with the(NH4)2SO4 gradient method.The encapsulation efficiency was determined by ultracentrifugation.With the encapsulation efficiency as index,the effect of the weight ratio of phospholipid to cholesterol(factor A),weight ratio of TMPP to phospholipid and cholesterol(factor B),hydration time(factor C)and concentration of(NH4)2SO4(factor D)on the preparation process were investigated by orthogonal design.Results The order of influence on encapsulation efficiency of TMPP-B liposomes was A D B C,and the optimum preparation technology conditions were A1B2C1D2.Three batches of TMPP-B liposomes were prepared according to the optimum technology conditions,the average particle size was(136.10±6.30)nm with uniform distribution,the average Zeta potential was(-35.70±3.60)mV,and the average encapsulation efficiency of TMPP was(73.14±0.71)%.Conclusion The liposomes prepared by this method have high encapsulation efficiency,uniform distribution,good morphology and stable quality.The method is simple and reasonable.

关 键 词：磷酸川芎嗪-冰片 脂质体 正交设计 制备工艺 

分 类 号：R932[医药卫生—生药学] R284.1[医药卫生—药学]