美沙拉嗪结肠靶向微丸的制备和体外评价

目的以结肠溶型丙烯酸树脂为包衣材料制备美沙拉嗪pH控制型结肠靶向微丸,评价其体外释药特性。方法挤出滚圆法制备美沙拉嗪微丸,采用L934正交设计实验优化工艺条件,流化床包衣机包衣,采用U884均匀设计试验优化工艺参数,考察了微丸圆整度、收率及体外释药特性。结果优化条件所得的微丸外观圆整,粒径分布均匀,收率高,在人工胃液中2h、人工小肠液中4h累计释放率<5%,人工结肠液1h累计释放率>95%,具有明显的结肠靶向释药特性。结论美沙拉嗪结肠靶向微丸具有良好的体外结肠靶向释药特性,可进一步进行体内释药行为考察。

Studies on preparation and dissolution test in vitro of mesalazine colon specific pellets

OBJECTIVE To prepare pH-dependent colonic-targeting pellets of mesalazine by coating with acrylic recin dissoluting in colon,and evaluate dissolution profiles in vitro.METHODS Mesalazine pellets was prepared by extrusion-spheronisation,the condition of techinics was optimized with the experiment of orthogonal design.The pellets was coated by coating maching of fluid bed.The parameter of techinics was optimized with the experiment of uniform design,the circularity,receipt rate and dissolution profiles was examed. RESULTS With optimized conditions,the pellets had round appearance,uniformly particle size distribution and high receipt rate.The cumulated release rate of the pellets were less than 5% in the artificial succus gastricus and intestinal juice,more than 95% in the artificial colonic juice.It could be concluded that the pellets assumed colonic-targeting release performance obviously.CONCLUSION Mesalazine colon specific pellets had good effect of colonic-targeting release in vitro and the release behavior in vivo need to be inspected.