基于SPG膜乳化法制备熊果酸微球的处方优化与体外释放研究  

Formulation optimization and in vitro release of ursolic acid microspheres prepared by SPG membrane emulsification

作　　者：王振霖 齐娜[1,2] WANG Zhen-lin;QI Na(Guilin Medical Institute,Guilin Guangxi 541004;Hospital of Integrated Western Medicine and Traditional Chinese Medicine,Southern Medical University,Guangzhou 510315)

机构地区：[1]桂林医学院,广西桂林541004 [2]南方医科大学中西医结合医院,广州510315

出　　处：《中南药学》2024年第3期641-646,共6页Central South Pharmacy

基　　金：广东省自然科学基金(No.2023A1515010570)。

摘　　要：目的制备熊果酸缓释微球,并考察其粒径、PDI、包封率、载药量以及体外释放。方法以熊果酸为模型药物、聚乳酸-羟基乙酸聚合物为载体材料,采用SPG膜乳化法制备熊果酸微球,通过单因素方法优化处方;纳米粒度测量仪测定粒径和PDI;光学显微镜观察形态;紫外-可见分光光度法测定熊果酸微球的体外释放率。结果制备的熊果酸微球粒径为(1.09±0.03)μm,PDI为(0.363±0.006),包封率为(87.19±4.71)%,载药量为(11.37±0.64)%,120 h体外累计释放率达到(80.53±2.82)%,无明显突释效应。结论熊果酸微球形态圆整,大小均一,包封率与载药量较高,体外无明显突释,工艺重现性好。Objective To prepare sustained-release microspheres containing ursolic acid and to determine their particle size,PDI,encapsulation efficiency,drug loading capacity,and in vitro release.Methods Ursolic acid microspheres were prepared as the model drug and polylactic acid hydroxyacetic acid polymer as the carrier material,with SPG membrane emulsification,and the formulation was optimized with a single factor method.The particle size and PDI were measured with a nanoparticle size analyzer,and the morphology under an optical microscope observed.The in vitro release rate of ursolic acid microspheres was determined by UV visible spectrophotometry.Results The particle size of ursolic acid microspheres was(1.09±0.03)μm,PDI was(0.363±0.006),entrapment efficiency was(87.19±4.71)%,drug loading was(11.37±0.64)%,and the cumulative release rate in vitro was(80.53±2.82)% after 120 h.Conclusion Ursolic acid microspheres have shape round,uniform size,high entrapment efficiency and drug loading,and are reproducible.

关 键 词：熊果酸 缓释微球 SPG膜乳化法 体外释放 

分 类 号：R94[医药卫生—药剂学] R283[医药卫生—药学]