尼群地平小丸的乳化溶剂扩散法制备

Preparation of Nitrendipine Pellets by Emulsion Solvent Diffusion Method

采用乳化溶剂扩散法,分别以羟丙甲纤维素邻苯二甲酸酯(HPMCP)和微粉硅胶为速释载体、EC和EudragitRSPO为阻滞剂制备了尼群地平的速释和缓释小丸。结果表明,当速释小丸中的尼群地平-HPMCP-微粉硅胶的比例达1∶2∶2以上时,溶出度迅速提高;X-射线衍射和差热分析结果表明速释和缓释小丸中药物结晶峰消失;所得小丸外观圆整,扫描电镜观察表明内部较致密,无药物的块状结晶,说明小丸中药物以无定形存在于固体分散体中。

Fast- and sustained-release pellets of nitrendipine (1) were prepared by emulsion solvent diffusionmethod using HPMCP and silica as fast release carriers, EC and Eudragit RS PO as retarding agents, respectively. Theresults showed that the dissolution from fast-release pellets was significantly increased when the ratio of 1-HPMCP-silicawas up to 1∶2∶2. The X-ray diffraction and differential thermal analysis results showed that the crystalline peak of 1 inboth pellets were disappeared, and there were no drug crystals on the surface of the pellets under scanning electron microscope.It was assumed that the drug was present in amorphous form in solid dispersion.