泮托拉唑钠肠溶缓释微丸的制备

Preparation of Sustained-Release and Enteric Coated Pellets of Pantoprazole

目的以丙烯酸树脂(Eudragit)为包衣材料,制备泮托拉唑钠(PAZ-Na)肠溶缓释微丸,并对其体外释药性能以及粉体学性质进行考察。方法采用溶液上药法(流化床底喷装置)制备PAZ-Na微丸,用Eudragit RS/RL作为缓释包衣材料,制备缓释微丸;用EudragitL100-55作为肠溶包衣材料,利用微型流化床进行包衣,制备肠溶缓释微丸,并通过单因素实验优化处方及其工艺条件,建立HPLC测定微丸中PAZ-Na,且测定了包衣微丸体外释放度。结果制备的肠溶缓释微丸质量良好,在pH1.2盐酸溶液中2h的释放度<10%;在PBS(pH6.8)中,释放曲线符合一级动力学方程,具有明显的缓释特征。结论PAZ-Na肠溶缓释微丸具有良好的体外缓释效果,制备工艺简单,重现性良好。

OBJECTIVE To prepare sustained release and enteric coated pellets ofpantoprazole-Na （PAZ-Na） with Eudragit as coating material, and study the release characteristics and the micromeritics. METHODS The drug-containing pellets were prepared in the fluid bed by solution layering and then coated in subminiature fluid bed with Eudragit RS/RL and Eudragit L100-55. The formulation of coating material was determined under single-factor investigation. A HPLC method was established to determine the release characteristics of PAZ-Na in vitro. RESULTS The drug-containing sustained release and enteric coated pellets were prepared. In the first 2 h, the coated pellets released less than 10% in pH 1.2 hydrochloric acid solution, and the curve of cumulative drug release was accorded with the first grade equation in PBS （pH 6.8）. The pellets showed sustained-release effect. CONCLUSION The coated pellets of PAZ-Na had a good effect of sustained-release in vitro, and the established process and formula were simDle and reDroducible.