论文部分内容阅读
目的 用生物可降解材料聚乳酸 (PDLLA)制备肺靶向红霉素缓释微球 (ERY PDLLA MS)。方法 用正交设计优化微球制备工艺 ,用扫描电子显微镜观察微球表面形态 ,差示扫描热分析确证含药微球的形成。并对所制备的红霉素微球的粒径及其分布、载药量、包封率、工艺重现性、体外释药、稳定性及在体内各组织的分布进行了研究。结果 微球形态圆整 ,且药物确已被包裹在微球中 ,而非机械混合。微球的平均粒径为 11.18μm ,粒径在 5～ 2 0 μm占总数的 94 %以上 ,载药量为 2 4 .16 % ,包封率为 6 3.5 4 % ,最佳工艺条件重现性良好 ,微球在 4℃及 2 5℃放置三个月各方面性质稳定 ,体外释药符合Higuchi方程Q =2 8.0 6 7+3.85 15t1/ 2 (r=0 .9834) ,动物体内实验表明 ,红霉素微球混悬剂较普通注射剂更聚集在肺组织。结论 微球制备工艺稳定 ,具有明显的缓释作用和肺靶向性
Objective To prepare lung targeting erythromycin sustained-release microspheres (ERY PDLLA MS) by using biodegradable material polylactic acid (PDLLA). Methods The preparation of microspheres was optimized by orthogonal design. The morphology of microspheres was observed by scanning electron microscopy. The formation of drug-containing microspheres was confirmed by differential scanning calorimetry. The particle size and distribution, drug loading, encapsulation efficiency, reproducibility, in vitro release, stability and the distribution of each tissue in the body of the prepared erythromycin microspheres were studied. As a result, the morphology of the microspheres was rounded and the drug was indeed encapsulated in the microspheres rather than mechanically mixed. The average particle size of the microspheres was 11.18μm, the particle size was 5 ~ 20μm, accounting for 94% of the total, the drug loading was 24.16% and the entrapment efficiency was 6 3.5% The microspheres were stable at 4 ℃ and 25 ℃ for three months. The in vitro drug release was in accordance with Higuchi’s equation Q = 2 8.06 7 + 3.85 15t1 / 2 (r = 0.9834) , Erythromycin microspheres suspension more concentrated than the average injection in the lung tissue. Conclusion Microspheres preparation process is stable, with significant sustained release and lung targeting