二氟沙星肺靶向微球制剂的制备

Preparation for lung targeted microsphere of Difloxacin

以可生物降解的明胶为载体,液体石蜡为油相,Span-80为乳化剂,选择正交设计优化空白明胶微球生产工艺,并考察其理化性质,采用乳化交联法制备二氟沙星肺靶向明胶微球。采用紫外可见分光光度计法,测定微球中二氟沙星的含量。结果表明,优选所制的二氟沙星肺靶向明胶微球形态圆整,表面光滑,平均粒径为8.33μm,粒径分布在5.0～25.0μm的微球达到95.71%,二氟沙星明胶微球包封率为62.43%,载药量为13.71%。采用动态分析法研究体外释药特性,二氟沙星明胶微球在12h处药物释放量达到65%,24h内药物释放量达到71%。制备工艺稳定可行,所得二氟沙星明胶微球具有良好的缓释效果。

The preparation technology was optimized by orthogonal experimental designed with biodegradable gelatin as the carrier, liquid paraffin as the oilphase, span-80 as the emulsifier, and Difloxacin loaded gelatin microsphere for lung targetting was prepared by the emulsion crosslinking method. Quantitative determination of Difloxacin was carried on by the method of UV spectrophotometry. and the optimal Difloxacin loaded gelatin microsphere was global with smooth surface, The arithmetic mean diameter of microsphere was 8.33 μm with 95.71% of microsphere which are ranging from 5.0 to 25.0 μm, total 62.43% for the encapsulation efficiency, and 13.71% for the drug loading, The release test in vitro showed that 65% of Difioxacin could release from gelatin microsphere in 12 h and 71% in 24 h with dynamic analysis. The preparation technology is good and stable, and the obtained microsphere can control the release of Difloxacin.