摘要
目的:制备琥珀酸美托洛尔微丸缓释片,并对其体外释药性质进行考察。方法:采用挤出-滚圆法制备载药丸芯,流化床包衣法制备缓释微丸,并将微丸与适当的辅料混合均匀后压制成片剂。考察微丸包衣增重、衣膜增塑剂柠檬酸三乙酯的用量及单硬脂酸甘油酯、微晶纤维素、乳糖等不同片剂稀释剂对药物释放的影响。结果:乙基纤维素水分散体包衣增重50%,柠檬酸三乙酯用量为15%时包衣微丸的释放效果良好;以单硬脂酸甘油酯为片剂稀释剂,与微丸比例为1∶1时,片剂的体外释药行为与微丸基本一致。1/4片、1/2片与整片之间有相似的释放特性。结论:制得琥珀酸美托洛尔微丸缓释片,其体外释药行为符合USP标准,制备工艺简便可行。
OBJECTIVE To prepare metoprolol succinate sustained-release pellet tablets, and to study their release behaviors in vitro. METHODS Metoprolol suceinate pellets were prepared using extrusion-spheronization equipment and coated by fluidized bed as bottom-spray. Coated pellets and appropriate excipients were mixed uniformly and then compressed to tablets. The effects of the pellets coating weight, the amount of triethyl citrate and the different tableting excipients（sueh as glyceryl monostearate, lactose, microcrys- talline cellulose） on release were evaluated. RESULTS When the coating weight was 50%and the amount of plasticizer was 15%, the release behavior of the pellets met the requirements. Using glyceryl monostearate as dituents （glyceryl monostearate and the pellets had the ratio of 1： 1）, the release behaviors in vitro of tablets consistented with pellets. The results showed that 1/4 tablet, 1/2 tablet and intact tablet had similar release characteristics. O3NCLUSION The preparation of metoprolol succinate sustained-release pellet tablets was simple and feasible, and the release behavior met USP standards.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2013年第21期1767-1771,共5页
Chinese Journal of Hospital Pharmacy
基金
河北省自然科学基金资助项目(编号:C2011206073)
关键词
琥珀酸美托洛尔
缓释微丸
流化床包衣
多单元缓释片
metoprolol succinate sustained-release pellets fluidized bed bottom-spray multi-unit sustained-release tablets
