环吡酮胺微海绵的制备工艺优化  

Optimization of Preparation Process of Ciclopirox Olamine Microsponges

作　　者：李媛媛 徐旭辉 张帅 李淼 董自波 LI Yuanyuan;XU Xuhui;ZHANG Shuai;LI Miao;DONG Zibo(School of Pharmacy,Jiangsu Ocean University,Lianyungang 222005;Jiangsu Marine Medicinal Resources Engineering Center,Lianyungang 222005)

机构地区：[1]江苏海洋大学药学院,江苏连云港222005 [2]江苏省海洋药用资源工程中心,江苏连云港222005

出　　处：《中国医药工业杂志》2023年第7期1082-1087,1111,共7页Chinese Journal of Pharmaceuticals

摘　　要：采用准乳液溶剂扩散法制备环吡酮胺(1)微海绵。采用单因素试验和Box-Behnken设计结合响应面法,探究聚合物(乙基纤维素)与1质量比、聚乙烯醇浓度、搅拌速度对微海绵包封率、得率的影响。优化得到的处方和工艺为:乙基纤维素与1质量比2.40∶1,聚乙烯醇浓度2.68%,搅拌速度350 r/min。优化的微海绵颗粒呈现出粒度分布较均匀的多孔道球状结构,体积平均径为(67.60±0.47)μm,面积平均径为(57.03±0.80)μm。在含30%聚乙二醇400的生理盐水中,1原料药在8h内累积释放率即达到(74.85±0.60)%,而1微海绵在48h内的累积释放率为(72.81±1.08)%,说明微海绵具有一定的缓释作用。Ciclopirox olamine(1)microsponges were prepared by quasi emulsion solvent diffusion method.The effects of mass ratio of polymer(ethyl cellulose)to 1,polyvinyl alcohol concentration and stirring speed on the encapsulation rate and yield of 1 microsponges were investigated with single factor test and Box-Behnken design combined with response surface methodology.The optimal formulation and process parameters were as follows:the mass ratio of ethyl cellulose to 1 was 2.40∶1,the concentration of polyvinyl alcohol was 2.68%,and the stirring speed was 350 r/min.The optimized microsponges had a porous spherical structure with uniform particle size distribution,the volume mean diameter and surface mean diameter were(67.60±0.47)and(57.03±0.80)μm,respectively.In saline containing 30%polyethylene glycol 400,the cumulative release rate at 8 h of the bulk drug reached(74.85±0.60)%,while the cumulative release rate at 48 h of 1 microsponges was(72.81±1.08)%,indicating that the microsponges had a certain sustained-release effect.

关 键 词：环吡酮胺 微海绵 BOX-BEHNKEN设计 响应面法 体外释放 

分 类 号：R944.9[医药卫生—药剂学]