Yang Zhen, Yu Jiankun, Yang Tianzi, Xing Haonan, Zhang Jinmin, Xian Lei, Ding Pingtian, Wang Dongkai
a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China and.
b Department of Basic Pharmaceutical Sciences , School of Pharmacy, Husson University , Bangor , ME , USA.
Pharm Dev Technol. 2016 Dec;21(8):943-950. doi: 10.3109/10837450.2015.1081612. Epub 2015 Aug 31.
The purpose of this study was to develop a method to prepare Metoprolol Succinate (MS) sustained release pellets and compress them into pellet-containing tablets without losing sustained release property. The drug layered pellets were coated with Eudragit NE 30D to obtain a sustained release (SR) property. The mechanical properties and permeability of the coating film were tailored by adjusting the proportion of talc in the coating dispersion and the weight gain of the coating film. Pellets with different MS release rates were tested and then mixed together by different ratios to optimize drug release rate. The mixed pellets were compressed into tablets with cushioning excipients. The results showed that when the ratio of talc and coating material was 1:4, the coating operation could be conducted successfully without pellet conglutination and the mechanical property of the coating film was enhanced to withstand the compress force during tableting. Blending SR-coated pellets of 20% weight gain with SR-coated pellets of 40% weight gain at the ratio of 1:5 could produce a constant and desired drug release rate. The formulation and the procedure developed in the study were suitable to prepare MS pellet-containing tablets with selected SR properties.
本研究的目的是开发一种制备琥珀酸美托洛尔(MS)缓释微丸并将其压制成含微丸片剂而不丧失缓释性能的方法。将药物层状微丸用Eudragit NE 30D包衣以获得缓释(SR)性能。通过调整包衣分散体中滑石粉的比例和包衣膜的增重,对包衣膜的机械性能和渗透性进行了调整。对具有不同MS释放速率的微丸进行测试,然后按不同比例混合在一起以优化药物释放速率。将混合后的微丸与缓冲辅料压制成片剂。结果表明,当滑石粉与包衣材料的比例为1:4时,包衣操作能够成功进行,微丸不会粘连,并且包衣膜的机械性能得到增强,能够承受压片过程中的压力。将增重20%的SR包衣微丸与增重40%的SR包衣微丸按1:5的比例混合,可以产生恒定且理想的药物释放速率。本研究中开发的配方和工艺适用于制备具有选定SR性能的含MS微丸片剂。