替米考星淀粉微球的制备及缓释性能的研究

Study on the Preparation and Drug Release of Tilmicosin Starch Microsphere Inclusion Compound

以可溶性淀粉为原料,N,N′-亚甲基双丙烯酰胺为交联剂,采用包埋法制备了替米考星淀粉微球,通过L9(34)正交试验设计,以载药量和包封率的综合得分为指标,优化了替米考星淀粉微球的制备工艺;分别用激光粒度分布仪、扫描电镜和综合热分析仪对载药微球进行了表征。结果表明最佳工艺条件为:淀粉4g、替米考星0.02g、交联剂0.95g、乳化剂0.75g、反应时间1h;影响因素的大小依次为:交联剂的质量>替米考星和淀粉的投料质量比>反应时间>乳化剂的质量;按优化工艺参数制得的载药微球的总载药量2.24%,包封率为89.6%;替米考星载药微球具有一定缓释效果,其制备方法合理可行。

Tilmicosin 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 through the L9（34） orthogonal experimental design and regression analysis based on the evaluation indicators of the drug loading and encapsulation efficiency.Tilmicosin starch microsphere inclusion compound was characterized by laser particle analyzer,scan electron microscope and thermogravimetric analysis（TGA）.The results indicated the best technological conditions was that：the quantity of soluble starch,tilmicosin,N,N′-methylene-bis-acrylamide and surfactant was 4,0.02,0.95,0.75g respectively and the reacting time was 1h.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 2.24% and 89.6% by optimizing conditions.The retarded release could be observed and this preparation method was reasonable and feasible.