右旋酮洛芬肠溶微丸的研制及其体外释放研究

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。

Preparation and in vtro Release of Dexketoprofen Enteric-coated Pellets

Objective： To prepare dexketoprofen enteric-coated pellets and explore the drug release rate respectively in 0. 1 mol·L- 1hydrochloric acid and phosphate buffered saline（ PBS,pH 6. 8）. Methods： Dexketoprofen enteric-coated pellets were prepared using fluid-bed coating technology,the blank sugar pellets were coated with drug layer,isolation layer and enteric layer in order. Drugloading rate as the index,the optimal concentrations of HPMC and drug were screened. Such indicators as adhesion,pellet uniform and surface color as the indices,the coating process was optimized by orthogonal experiment. Drug release in PBS of the enteric-coated pellets and the common enteric-coated tablets were compared. Results： The prepared pellets showed the properties of uniform drug loading,high drug-loading rate,complete round shape and lustrous appearance. The concentration of HPMC and drug was 5% and 15%,respectively. The optimal coating process was as follows： the material temperature was 36℃,the atomization pressure was 1. 0 bar and the airbrush rate was 0. 8 ml·min- 1. The drug release of the pellets in hydrochloric acid was below 10% in 2 hours,while the release in PBS was greater than that of the common enteric-coated tablets. Conclusion： The prepared enteric-coated pellets are feasible in technology,and exhibit satisfactory acid endurance and drug release in vitro.