玻璃体注射用秦皮甲素微球的处方及制备工艺优化  

Optimization of Formulation and Preparation Process of Intravitreally Injectable Esculin-loaded Microspheres

作　　者：罗芮 雷芳 费清松 何宁[1,2,3,4] LUO Rui;LEI Fang;FEI Qing-song;HE Ning(Department of Pharmaceutics,College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China;Institute of Pharmaceutics,Anhui Academy of Chinese Medical Sciences,Hefei 230012,China;Anhui Province Key Laboratory of Pharmaceutical Preparation Technology and Application,Hefei 230012,China;Engineering Technology Research Center of Modernized Pharmaceutics,Education Office of Anhui Province,Hefei 230012,China)

机构地区：[1]安徽中医药大学药剂系,合肥230012 [2]安徽省中医药科学院药物制剂研究所,合肥230012 [3]安徽省药物制剂技术与应用重点实验室,合肥230012 [4]安徽省教育厅现代药物制剂工程技术研究中心,合肥230012

出　　处：《中国药学杂志》2022年第9期729-735,共7页Chinese Pharmaceutical Journal

基　　金：安徽省自然科学基金资助(2108085MH312);安徽省“特支计划”创新领军人才项目资助。

摘　　要：目的研究玻璃体注射用秦皮甲素微球的制备工艺并对其进行优化。方法以秦皮甲素为模型药物,壳聚糖为载体材料,采用乳化交联法制备秦皮甲素微球,在单因素考察的基础上,通过星点设计进行处方工艺优化,从而得到秦皮甲素微球最佳制备条件。结果制备所得秦皮甲素微球呈淡黄色粉末状态,外观圆整,能均匀分散于5 mg·mL^(-1)的羧甲基纤维素钠溶液中,其载药量为8.03%,包封率为93.03%,平均粒径为4.81μm。结论本研究制备得到的秦皮甲素微球具有较佳的载药量和包封率,且粒径符合玻璃体注射要求,可为黄斑病变的治疗提供新的剂型。OBJECTIVE To optimize the prescription and preparation process of intravitreally injectable esculin-loaded microspheres.METHODS Esculin-loaded chitosan microspheres were prepared by emulsion chemical cross-linking method with esculin as a model drug and chitosan as carrier material.Based on the result of a single factor test,central composite design and response surface methodology was further adopted to optimize preparation technology.Thus,the optimal formulation and technology of esculin-loaded microspheres were obtained.RESULTS The esculin-loaded microspheres obtained by central composite design and response surface methodology are in the state of light yellow powder,with round appearance,and can be evenly dispersed in 5 mg·mL^(-1) sodium carboxymethyl cellulose solution.And its drug loading is 8.03%,the entrapment efficiency is 93.03%,the particle size is 4.81μm.CONCLUSION The prepared esculin-loaded microspheres had good drug loading and entrapment efficiency,and the particle size met the requirements of vitreous injection,it can provide a new dosage form for the treatment of macular degeneration.

关 键 词：秦皮甲素 壳聚糖微球 乳化交联法 星点设计-响应面优化法 

分 类 号：R944[医药卫生—药剂学]