琥珀酸美托洛尔缓释微丸型片剂的制备与体外释放度考察

Preparation and in vitro Release of Metoprolol Succinate Sustained-release Pellet Tablets

目的制备琥珀酸美托洛尔缓释微丸型片剂,并对其体外释放度进行考察。方法采用流化床包衣法制备琥珀酸美托洛尔缓释微丸,将缓释微丸与适合的辅料混合后采用直接压片法制备琥珀酸美托洛尔微丸型片剂,并采用f2相似因子法评价自制制剂和参比制剂在释放介质中的体外释放行为。结果选用空白蔗糖丸芯粒径为250~350μm,以Kollicoat SR 30D为微丸的衣膜材料,包衣增重为20%,增塑剂用量为20%,滑石粉用量为50%,压片压力为80 kN时,自制制剂和参比制剂f2相似因子值大于50,说明2种制剂体外释放行为相似。结论制备的琥珀酸美托洛尔缓释微丸型片剂的释药行为较好,有望应用于工业生产。

Objective To prepare metoprolol succinate sustained-release pellet tablets,and to investigate their in vitro drug release behavior. Methods Metoprolol succinate sustained-release pellets were prepared by fluid bed coating technology,while the sustained-release pellet tablets were prepared by direct compression of sustainedrelease pellets and suitable excipients. The release behavior similarity was investigated between the reference and self-prepared tablets in release media. Similar factor（ f2） was used to evaluate the similarity of release curves. Results The size of blank sugar pellets was 250- 350 μm. With Kollicoat SR 30 D as the coating material,the coating level was 20%,the plasticizer content was 20%,the anti-tacking agent content was 50%,and the tableting pressure was 80 kN. The value of f2 was more than 50,and the release behavior was similar. Conclusion The release behavior of metoprolol succinate sustained-release pellet tablets is quite satisfactory. This method of preparation may be used in industrial production.