摘要
目的利用热熔挤出技术制备硝苯地平固体分散体,以增加其溶出速度和溶出度。方法分别以PVP-VA64、PVP-S630和Soluplus为载体采用热熔挤出技术制备固体分散体;利用热分析法、X-射线粉末衍射、扫描电镜和红外光谱进行表征,并按照《中华人民共和国药典》的方法测定了硝苯地平、硝苯地平与载体的物理混合物以及硝苯地平固体分散体的体外溶出度。结果硝苯地平以无定形状态存在于以PVP-VA64和PVP-S630为载体制备的固体分散体中,溶出速率和溶出度远高于以Soluplus为载体的固体分散体。结论利用热熔挤出技术,以PVP-VA64和PVP-S630为载体制备的固体分散体可以显著提高硝苯地平的溶出速率和溶出度。
Objective To prepare and characterize solid dispersions of nifedipine with PVP-VA64,PVP-S630 and Soluplus with the intention to improve the dissolution profiles of nifedipine. Methods The solid dispersions were prepared by hot-melt extrusion. The properties of the solid dispersions was evaluated by DSC, XPRD, IR, SEM and dissolution studies. Results The results indicated that nifedipine was in the amorphous state when dispersed in the SD-VA64 or SD-S630, and partially in microcrystal state in the SD-Solu. The solid dispersions of nifedipine with PVP-VA64 and PVP-S630 markedly enhanced drug dissolution compared with pure nifedipine, physical mixture. Conclusions Dissolution of nifedipine was improved in solid dispersion using PVP-VA64 and PVP-S630 prepared by hot-melt extrusion.
出处
《中国药剂学杂志（网络版）》
2014年第6期177-184,共8页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
固体分散体
硝苯地平
热熔挤出
pharmaceutics
solid dispersion
nifedipine
hot-melt extrusion
