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No entire nitrendipine crystals were observed visually in SEM photos. The results of X-ray diffraction and differential scanning calorimetry analysis indicated that the crystalline form of nitrendipine was highly dispersed in microspheres, so as amorphous state. The drug release rate of microspheres could be controlled with adjusting the ratio of solid dispersion carriers and retarding agents formulated. The agitation speed and temperature of the preparation process have distinct effect on micromeritic properties of microspheres. The release profiles of the microspheres were mainly affected by the stirring rate of paddle, the concentration of SDS and pH of dissolution medium. Cooling speed and time, however, have no evident influence on the drug release rate of the microspheres. The dissolution data showed that the mechanism of drug release from microsphers was mainly diffusion-controlled. The incorporation efficiencies of 3 batches sample were exceed 96. 8%, which implied that the current method was suitable for design sustained-release dosage form for poorly water-soluble drug.
在扫描电子显微镜下观察,在微球内外未发现尼群地平的完整结晶,X-射线粉末衍射和差示扫描量热试验结果也显示,尼群地平已经被高度分散在微球中;微球的释药速度可通过调整处方中固体分散体载体和阻滞剂的比例控制;制备温度和搅拌速度对微球的质量影响较大;溶出仪的搅拌速度,释放介质的浓度和pH对微球的释放有较大的影响;制备过程中的冷却速度和冷却时间对微球的释放行为影响不很明显;方程拟合的结果表明缓释微球的释药行为符合扩散机制;测定三批微球样品的包封率均在96.8%以上,表明该法适合于制备难溶性药物的缓释微球。