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目的:制备右旋酮洛芬肠溶微丸,并考察其在0.1 mol·L-1盐酸溶液和pH 6.8磷酸缓冲液(PBS)中的释放情况。方法:采用流化床包衣技术,在空白糖丸芯上依次包主药层、隔离层和肠溶衣层,制备成肠溶衣微丸;以上药率为指标,考察HPMC浓度和主药上药浓度;观察是否粘连、颗粒大小均一度和表面色泽均匀与否等综合指标,采用正交试验优选包衣工艺条件;与普通肠溶片比较在PBS中的释放情况。结果:制得的微丸上药均匀、上药率高、外观圆整有光泽;确定HPMC浓度和主药上药浓度分别为5%和15%,优选出最佳包衣工艺条件为物料温度为36℃、雾化压力为1.0 bar及喷枪速度为0.8 ml·min-1;在盐酸溶液中2 h的释放量小于10%,在PBS中的释放度高于普通肠溶片。结论:所制右旋酮洛芬肠溶微丸工艺可行,具有良好的耐酸性和体外释放度。
OBJECTIVE: To prepare dexketoprofen enteric-coated pellets and investigate its release in 0.1 mol·L-1 hydrochloric acid and pH 6.8 phosphate buffered saline (PBS). Methods: Using fluidized bed coating technology, enteric coated pellets were prepared by packing the primary drug layer, the isolation layer and enteric coating layer on the blank confectionery core. The above drug rates were taken as indexes to investigate the effect of HPMC concentration and main drug On the drug concentration; observe whether the adhesion, particle size uniformity and surface color uniformity or not and other comprehensive indicators, the orthogonal test to optimize the coating process conditions; compared with ordinary enteric-coated tablets in PBS release. Results: The prepared pellets were uniformly coated on the drug, the drug rate was high, the appearance of a round and shiny; determine the HPMC concentration and the drug concentration on the main drug were 5% and 15%, respectively, preferably the best coating process conditions for the material temperature 36 ℃, atomization pressure of 1.0 bar and gun speed of 0.8 ml · min-1. The release of 2 h in hydrochloric acid solution was less than 10%, and the release rate in PBS was higher than that of ordinary enteric-coated tablets. Conclusion: The process of dexketoprofen enteric-coated pellets is feasible and has good acid resistance and in vitro release.