双氯芬酸钠淀粉微球的制备及其质量评价  

Preparation and Quality Evaluation of Starch Microspheres of Diclofenac Sodium

作　　者：隋小宇[1] 张琳[1] 刘畅[1] 袁橙[1] 马晓星[1] 刘婷婷[1] 韩翠艳[1] 黄海涛[1] 

机构地区：[1]齐齐哈尔医学院药学院,黑龙江齐齐哈尔161006

出　　处：《中国药学杂志》2016年第7期554-560,共7页Chinese Pharmaceutical Journal

基　　金：齐齐哈尔市科学技术计划项目(SFGG-201340)

摘　　要：目的以可溶性淀粉为原料,N,N'-亚甲基双丙烯酰胺为交联剂,双氯芬酸钠为主药,通过反相乳化交联法制备双氯芬酸钠载药淀粉微球。方法以微球平均粒径和包封率为指标,采用单因素及正交实验优化微球的处方和制备工艺。采用光学显微镜、透射电镜、红外光谱仪及差热分析仪对所获微球的外观和结构进行表征,并通过透析法对载药微球的体外释药情况进行考察。结果经正交实验优化后的制备条件为:淀粉浓度10%,交联温度55℃,交联剂用量0.2 g,油水体积比5∶1,乳化剂用量5 m L,交联时间60 min,此条件制得的淀粉微球平均粒径为9μm,形状近球形,包封率为67.52%。红外光谱和差热分析表明淀粉已发生交联。结论载药淀粉微球具有较好的缓释作用,药物的体外释放符合Weibull方程。OBJECTIVE To prepare starch microspheres of diclofenac sodium by inverse crosslink emulsification method.METHODS Mean particle size and encapsulation efficiency of starch microspheres were used as indicators,single factor and orthogonal design methods were performed for optimizing preparation process and formulations of starch microspheres. The appearance and structure of the microspheres were researched by optical microscope,transmission electron microscope,infrared spectroscopy and differential thermal analyzer. In vitro drug release behavior was investigated by dialysis method. RESULTS The preparation conditions optimized by orthogonal design： the concentration of starch 10%,crosslinking temperature 55 ℃,dosage of cross-linking agent 0. 2 g,the volume ratio of oil phase and water 5 ∶ 1,amount of emulsifier 5 m L,cross-linking time 60 min. Starch microsphere obtained by above condition has an average particle size of 9 μm,appearance is irregular spherical shape,and encapsulation efficiency was67. 52%. Results of IR spectra and DTA curves showed that starch cross-links have happened. CONCLUSION In vitro releasing curve showed that the diclofenac sodium starch microspheres have good sustain release effect,drug release complies with the Weibull equation.

关 键 词：双氯芬酸钠 淀粉微球 乳化交联法 包封率 体外释药 

分 类 号：R944[医药卫生—药剂学]