白藜芦醇-泊洛沙姆188固体分散体的制备及其性能研究  

Preparation and Properties of Resveratrol-poloxamer 188-solid Dispersion

作　　者：任红暖 王晓丽[1] 陈肖如 陈丽萍[1] 周婷婷[1] 高振珅[1,2] 宋兴良[2,3,4] 

机构地区：[1]临沂大学药学院,山东临沂276005 [2]临沂大学现代中药研究所,山东临沂276005 [3]临沂大学化学化工学院,山东临沂276005 [4]山东省资源与环境分析化学重点实验室,山东临沂276005

出　　处：《中国药房》2015年第25期3554-3557,共4页China Pharmacy

基　　金：大学生创新创业计划项目资助;项目编号为201410452021;指导教师为高振珅;宋兴良

摘　　要：目的:制备白藜芦醇-泊洛沙姆188固体分散体(RES-P188-SD),并对其体外溶出特性及抑菌性进行研究。方法:以P188为载体,采用溶剂法制备RES-P188-SD。以药物与载体质量比、熔融温度、筛孔目数为考察因素,以RES溶解度与收率为考察指标,设计L9(34)正交试验优选其制备工艺。以考察指标的综合评分进行结果分析,并进行验证试验。根据最优工艺制备RES-P188-SD后采用篮法测定其溶出度并计算累积溶出度,扫描电镜法分析物相表征,管碟法测定其抑菌性。结果:最优工艺为药物与载体质量比1∶10,熔融温度70℃,筛孔目数80目。按最优工艺所制样品的平均溶解度为0.51 mg/ml(RSD=1.96%,n=3),平均收率为91%(RSD=0.64%,n=3),15 min的平均累积溶出度即达83%(RSD=0.69%,n=3);其药物以非晶形式均匀分散在载体中;RES-P188-SD对金黄色葡萄球菌和大肠埃希菌均有抑制作用。结论:优选工艺稳定、可行。成功制得RES-P188-SD,可为提高RES的溶解度、溶出速率及抑菌性提供依据。OBJECTIVE：To prepare Resveratrol-poloxamer 188-solid dispersion（RES-P188-SD）and study its dissolving characteristic in vitro and antibacterial activity. METHODS： With P188 as the carrier, solvent method was used to prepare RES-P188-SD. With the mass ratio of drug to carrier,melting temperature and mesh number as the observed factors,and solubility and yield of RES as the observed indexes,L9（34）orthogonal test was designed to optimize the preparation technology,and comprehensive score of observed indexes were analyzed. The verification test was carried out. After RES-P188-SD was prepared by the optimal technology,basket method was used to determine its dissolution rate and then its accumulative dissolution rate was calculated,scanning electron microscopy to analyze phase characterization and cylinder-plate method to determine antibacterial activity. RESULTS：The optimal technology was as follows as the mass ratio of drug to carrier of 1 ∶ 10,melting temperature of 70 ℃ and mesh number of 80. For the sample prepared by the optimal technology,average solubility was 0.51 mg/ml（RSD=1.96%,n=3）,average yield was 91%（RSD=0.64%,n=3）,average 15 min accumulative dissolution rate was up to 83%（RSD=0.69%,n=3）;the drug in amorphous form was homogenously distributed in the carrier;RES-P188-SD could inhibit Staphylococcus aureus and Escherichia coli. CONCLUSIONS：The optimal technology is stable and feasible,by which RES-P188-SD has been prepared successfully,providing reference for increasing the solubility,dissolution rate and antibacterial activity of RES.

关 键 词：白藜芦醇 泊洛沙姆188 固体分散体 溶解度 抑菌性 

分 类 号：R944.9[医药卫生—药剂学]