氟苯尼考淀粉微球的制备及缓释性能的研究

Study on the preparation and drug release of florfenicol starch microsphere inclusion compound

以可溶性淀粉作为原料,N,N′-亚甲基双丙烯酰胺为交联剂,采用包埋法制备了氟苯尼考淀粉微球,通过响应曲面实验设计,以载药量和包封率的综合得分为指标,优化了氟苯尼考淀粉微球的制备工艺;并进一步采用体外动态释药法评价其释药特征;分别用激光粒度分布仪和扫描电镜对载药微球进行了表征。结果表明最佳工艺条件为:淀粉4g、氟苯尼考0.18g,交联剂0.94g,反应时间1.46h;影响因素的大小依次为:氟苯尼考质量>交联剂用量>反应时间;按优化工艺参数制得的载药微球载药量28.1%,包封率为64.2%;氟苯尼考淀粉微球体外释药规律符合一级释放方程和Korsmeyer-Peppas模型方程;氟苯尼考载药微球具有一定缓释效果,其制备方法合理可行。

Florfenicol starch microsphere were synthesized with soluble starch as material and N,N′-methylene-bis-acrylamide as crosslinking agent by using pack cementation method. The preparation process was optimized by Response Surface Methodology based on the evaluation indicators of the drug loading and encapsulation efficiency. The constant temperature vibration dialysis method was carried out to evaluate theophylline release from florfenicol starch microspheres inclusion compound in vitro. Florfenicol starch microsphere inclusion compound was characterized by laser particle analyzer and scan electron microscope. The results indicated the best technological conditions were that：the quantity of soluble starch,tilmicosin and N,N′-methylene-bis-acrylamide were 4g,0.18g,0.94g respectively,and the reacting time was 1.46h. Influence factors were the quantity of N,N′-methylene-bis-acrylamide,the quantity ratio of tilmicosin to soluble starch,the reacting time,the quantity of emulsifier in order. The drug loading and embedding ratio were respective 28.1% and 64.2% by optimizing conditions. The drug release profile could be described by first-order release equation and Korsmeyer-Peppas equation. The retarded release could be observed and this preparation method was reasonable and feasible.