【摘要】 目的采用喷雾干燥法、冷冻干燥法及共沉淀法3种工艺制备尼群地平/PVPk25固体分散体,比较3种不同工艺制得尼群地平固体分散体的性质。方法通过扫描电镜(SEM)、差示扫描量热(DSC)、粉末X-射线衍射(PXRD)和傅里叶红外光谱(FT-IR)等技术分析尼群地平固体分散体的微观形态特征、药物的晶体特征及分子间相互作用。通过溶出仪及恒温摇床分别考察不同工艺制备尼群地平固体分散体的溶出性质及溶解度特征。通过超饱和抑晶实验考察聚合物对超饱和状态下药物结晶的抑制效应。结果喷雾干燥法所制得的固体分散体中,尼群地平以无定型形式状态存在。相比共沉淀法及冷冻干燥法,喷雾干燥法制得的固体分散体显著地促进了尼群地平的溶出及溶解度(P<0.05)。超饱和结晶抑制实验结果显示,PVPk25可以明显抑制超饱和状态下尼群地平的结晶。结论基于以上性质分析可知,喷雾干燥技术所制得的尼群地平固体分散体性质最佳。喷雾干燥技术更适合于实际生产及产业化应用。更多还原

【Abstract】 OBJECTIVE To compare the properties of nitrendipine/PVP k25 solid dispersions prepared by three different technologies including spray drying,freeze-drying and co-precipitation technology. METHODS The characteristics of nitrendipine solid dispersions including micromorphology,crystalline profile and intermolecular interactions were analyzed by scanning electron microscopy( SEM),differential scanning calorimetry( DSC),powder X-ray diffraction( PXRD) and Fourier transform infrared spectroscopy( FT-IR). The dissolution and solubility characteristics were investigated by dissolution apparatus and constant temperature shaker. The crystallization inhibition effect of polymers against the drug in a supersaturated state was investigated by supersaturation crystallization experiment. RESULTS Nitrendipine existed in an amorphous form in the solid dispersion obtained by spray drying method. Compared with co-precipitation and freeze-drying method,the solid dispersion prepared by spray drying method significantly improved the dissolution and solubility of nitrendipine( P < 0. 05). The results of supersaturation crystallization inhibition test showed that PVP k25 could obviously inhibit the crystallization of nitrendipine in supersaturated state. CONCLUSION Based on the analysis of the above mentioned properties,nitrendipine solid dispersion prepared by spray drying technology displays the most optimal properties. Spray drying technology is more suitable for the practical production and industrial applications of nitrendipine solid dispersions.更多还原