伊曲康唑固体脂质纳米粒的制备  

Study on Preparation of Itraconazole Solid Lipid Nanoparticles

作　　者：丁艳 武夏明[2] 黄桂华[3] 

机构地区：[1]山东省医药技师学院,山东泰安271016 [2]泰山医学院附属医院 [3]山东大学药学院

出　　处：《中国药师》2012年第8期1124-1128,共5页China Pharmacist

摘　　要：目的:制备伊曲康唑固体脂质纳米粒,并考察其理化性质。方法:采用乳化-低温固化法制备伊曲康唑固体脂质纳米粒(ITZ-SLN);在脂质、表面活性剂等辅料和主药用量的单因素考察基础上,以包封率为评价指标,采用正交试验设计,优化处方组成和制备工艺;用低温超速离心法测定包封率,透射电镜观察形态,激光粒径分析仪测定粒径和ξ电位。结果:脂质、表面活性剂和主药的用量对ITZ-SLN包封率均有不同程度的影响。以优化处方制备的伊曲康唑固体脂质纳米粒为类球形实体,粒径分布比较均匀,平均粒径为dav=(118.2±15.00)nm,ξ电位(-37.06±0.53)mV,包封率(92.11±1.60)%。结论:乳化-低温固化法制备伊曲康唑固体脂质纳米粒工艺可行。Objective： To prepared itraconazole solid lipid nanoparticles （ITZ-SLN） and investigate the physicochemical properties. Method： ITZ-SLN was prepared by emulsification -low temperature solidification method. Based on the results of the single factor test with the amount of adjuvants and itraconazole as the indices, the formula and the preparation conditions were optimized by orthogonal experiments using the entrapment efficiency as the evaluation index. The entrapment efficiency was determined by low temperature - ultracentrifugation. An electron microscope was used to observe the morphology of ITZ -SLN. A laser particle size analyzer was applied to study the particle diameter and potential of ITZ-SLN in suspension. Result： The amount of lipid, surfactant and itraconazole showed different extent of influence on the entrapment efficiency of ITZ-SLN. ITZ-SLN prepared with the optimized formulation was spherical shape with the mean diameter （ dav ） of （ 118.2±15.00） nm and the potential of （ - 37.06± 0.53 ） mV. The average entrapment efficiency was （92.11± 1.60） %. Conclusion： The emulsification-low temperature solidification method is feasible for the preparation of ITZ-SLN.

关 键 词：伊曲康唑 固体脂质纳米粒 制备 乳化-低温固化法 

分 类 号：R944.9[医药卫生—药剂学]