局部用环孢素聚乳酸微球的制备  

Preparation of cyclosporin A polylactic acid microsphere for topical application

作　　者：梁志波[1] 刘锟[1] 吴红[2] 赵晋波[1] 李小飞[1] 

机构地区：[1]第四军医大学唐都医院胸外科,陕西西安710038 [2]第四军医大学药学系化学教研室,陕西西安710032

出　　处：《医学研究生学报》2007年第5期490-493,497,I0002,共6页Journal of Medical Postgraduates

基　　金：国家自然科学基金资助项目(批准号:39970707);陕西省自然科学基金资助项目(批准号:99SM37)

摘　　要：目的：采用O／W型乳化-溶剂挥发法制备环孢素聚乳酸微球，并对微球性状进行考察。方法：通过正交设计试验筛选其最佳制备工艺，用扫描电镜观察微球表面形态。采用激光粒径分析仪对微球的平均粒径分布检测，并通过高效液相色谱对微球的载药量、包封率、体外释药性能进行了研究。结果：应用通过正交设计筛选后的制备工艺，所得到环孢素聚乳酸微球的形态圆整，平均粒径为18．234μm，粒径在9．525～32．400μm的占总数的80％以上。包封率为（86．12±0．77）％，载药量为（34．51±0．63）％。环孢素-聚乳酸微球的体外释药情况为30d，累积释药量为40．8％，在释放前期释放速率较快，5d后释放变得平稳。结论：可获得较满意的环孢素聚乳酸微球制备工艺，且微球具有明显的缓释性能。Objective：To prepare the cyclosporin A （CsA） polylactic acid microspheres using solvent evaporation method from an oil-in-water system. Methods：Orthogonal experiment was used to optimize the method of CsA polylactic acid microspheres preparation. The microspheres were characterized for drug loading and entrapment efficiency by high-performance liquid chromatography （HPLC）, average size by particle size analyser and surface morphology by scanning electron microscopy （SEM）. In vitro the release kinetics were studied using a modified dialysis method. Results：SEM studies showed discrete and spherical particles with smooth surfaces. The average particle size was 18. 234 μm, with more than 80% of the microspheres falling in the range of 9. 525 - 32. 400 μm. The drug loadings ranging was （34.51 ±0.63） % with a high encapsulation efficiency （86.12 ± 0. 77） % determined by HPLC. In vitro release study revealed a profile of sustained release of CsA from CsA-PLA-MS. The accumulated release percentage of CsA microspheres were 40.8% in 30 d. CsA release profiles show CsA release could be divided by two different phases, fast release within the first few days and the subsequent sustained release. Conclusion：CsA polylactic acid microspheres have been successfully prepared and sustained release of CsA from microspheres have been achieved.

关 键 词：环孢素A 聚乳酸 微球 局部应用 

分 类 号：R943[医药卫生—药剂学]