尼群地平缓释微丸的制备及体外释放影响因素考察

Preparation of Nitrendipine Sustained-release Pellets and the Influencing Factors

目的:对影响尼群地平缓释微丸中药物体外释放的制备工艺因素进行考察。方法:采用挤出滚圆法制备尼群地平缓释微丸,通过体外释放度试验,对影响缓释微丸中药物释放的润湿剂乙醇浓度及用量、挤出速度、滚圆转速及滚圆时间等因素进行考察,优化制备工艺条件。结果:润湿剂用量及乙醇浓度对药物体外释放影响显著,乙醇浓度应在35%以下,用量宜控制在44mL左右。挤出速度、滚圆转速及滚圆时间等对药物体外释放有一定的影响,分别以48r.min-1、1400r.min-1、5min为宜。结论:采用上述制备工艺,可制得释药速度符合要求的尼群地平缓释微丸。

OBJECTIVE： To investigate the technological factors that influence the drug release of nitrendipine sustained- release pellets. METHODS： The nitrendipine sustained- release pellets were prepared by extrusion- spheronization technology. By means of in vitro drug release test, the factors that influence the drug release including the amount of the wetting agent and the concentration of ethanol,, extrusion speed, spheronisation speed and spheronisation time were investigated to optimize the technological conditions. RESULTS： The amount of the wetting agent and the concentration of ethanol had significant effects on drug release. The optimal concentration of ethanol was less than 35% and the optimal amount of the wetting agent was about 44 mL. Extrusion speed, spheronisation speed and spheronisation time had certain effects on drug release, and their optimal values were 48 r ·min^-1, 1 400 r · min^-1 and 5 min, respectively. CONCLUSION： The nitrendipine sustained - release pellets prepared in the above - mentioned technological conditions are up to the standard in drug release velocity.