【摘要】 目的采用乳化溶剂蒸发法制备环丙沙星聚乳酸微球,并对其性状进行考察。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,并对微球的平均粒径、载药量、包封率、体外释药性能进行了研究。结果环丙沙星聚乳酸微球的形态圆整,且药物确已被包裹在微球中,微球的平均粒径为28080±015μm,粒径在250-390μm之间的占总数的90%以上。包封率为685%±058,载药量为341%±051,环丙沙星微球的体外释药情况为532小时的累积释药量为840%,T1/2为319h,Higuchi方程为Q=-00043+00039t1/2,r=09941。结论本研究获得了较满意的制备环丙沙星聚乳酸微球的工艺,且微球的体外释药性能具有明显的缓释效果。更多还原

【Abstract】 Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were prepared using solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonal experiment was used to optimize the method of CFX-PLA-MS preparation. Microspheres were characterized in terms of morphology, size, encapsulation efficiency, drug loading and in vitro drug release. Results The physical state of CFX-PLA-MS was determined by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). Microspheres formed were spherical with smooth surfaces. Drug was enveloped in microspheres without mixing physically with PLA. The average particle size was 280.80±0.15 μm, with over 90% of microspheres falling in the range of 250-390 μm. The encapsulation efficiency was 65.8%±0.58% and the drug loading was 34.1%±0.51%. In vitro release study revealed a profile of sustained release of ciprofloxacin from CFX-PLA-MS. The accumulated release percentage and half-life (T_ 1/2) of ciprofloxacin microspheres were 84.0% in 53.2 h, and 31.9 h, respectively. Higuchi equation was Q=-0.004 3 + 0.003 9 t 1/2, r=0.994 1. Conclusion Ciprofloxacin microspheres have been successfully prepared and sustained release of CFX from microspheres is achieved.更多还原