不同工艺制备尼群地平固体分散体的性质比较研究

发布时间：2018-04-22 02:08

本文选题：尼群地平 + 固体分散体　；参考：《中国药学杂志》2017年10期

【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(P0.05)。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。
[Abstract]:Objective to prepare nitrendipine / PVPk25 solid dispersion by spray drying, freeze-drying and co-precipitation, and to compare the properties of nitrendipine / PVPk25 solid dispersion prepared by three different processes. Methods scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR) were used to analyze the microscopic morphology, crystal characteristics and intermolecular interaction of nitrendipine solid dispersions. The dissolution properties and solubility characteristics of nitrendipine solid dispersion prepared by different processes were investigated by means of dissolution apparatus and constant temperature rocker. The inhibition effect of polymer on drug crystallization in supersaturated state was investigated by supersaturation inhibition experiment. Results in the solid dispersion prepared by spray drying, nitrendipine existed in an amorphous state. Compared with co-precipitation method and freeze-drying method, the solid dispersion prepared by spray drying significantly promoted the dissolution and solubility of nitrendipine. The results show that PVPk25 can inhibit the crystallization of nitrendipine in supersaturated state. Conclusion based on the above analysis, the properties of nitrendipine solid dispersion prepared by spray drying are the best. Spray drying technology is more suitable for practical production and industrial application.
【作者单位】：吉林医药学院药学院;吉林大学生命科学学院;北京大学药学院;
【基金】：国家自然科学基金资助项目(81602654) 中国博士后科学基金面上项目(2015M571374) 吉林省科技发展计划项目(20160520046JH) 吉林省教育厅资助项目(吉教科合字2015第401号) 2015年吉林省大学生创新创业课题
【分类号】：R943

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