摘要
目的制备普瑞巴林胃滞留缓释片,对其体外释药机理进行探讨。方法以溶出相似因子f_2、处方流动性、膨胀性能作为考察指标,通过单因素和正交设计筛选得到最优处方,并对最优处方进行释药机理研究。结果最优处方为含有普瑞巴林165mg,缓释骨架材料40%(尤特奇RS PO∶HPMC K100M=3∶1),凝胶剂卡波姆71G 4%,崩解剂交联聚维酮XL 30. 75%,溶胀剂聚氧乙烯N60K 10. 33%,硬脂酸镁适量。普瑞巴林缓释片的释放机理主要为溶蚀同时有部分为Fick's扩散。结论本研究制备的普瑞巴林胃滞留缓释片操作简单,体外释药行为理想,为普瑞巴林缓释制剂的开发提供了参考。
OBJECTIVE To prepare pregabalin gastric retention sustained-release tablets and investigate the in vitro release mechanism of drug. METHODS The formulation of Pregabalin sustained-release tablets was optimized in terms of f2, liquidity and expansive property by single factor test and orthogonal design.The release mechanism of tablets was studied. RESU LTS The optimal formulation contained matrix material 40% （Eudragit RSPO∶HPMC K100M=3∶ 1）,Carbomer 71G 4%,PVPP XL 30.75%,PEO N60K 10.33%
and magnesium stearate of appropriate amount.The prevailing release mechanism was erosion with diffusion as a supplementary release mechanism. CONCLUSION Pregabalin sustained-release tablets prepared in this study showed ideal drug release behavior,which can be used as a reference for the development of pregabalin sustained-release preparations.
作者
史雯星
尹莉芳
祝玲
陈玉红
石心红
SHI Wen-xing;YIN Li-fang;ZHU Ling;CHEN Yu-hong;SHI Xin-hong(China Pharmaceutical University,Nanjing 211198,China)
出处
《海峡药学》
2018年第10期9-13,共5页
Strait Pharmaceutical Journal
关键词
普瑞巴林
缓释片
制备
释药机理
Pregabalin
Sustained-release tablets
Preparation
Drug release mechanism
