致孔剂调节布地奈德肠溶缓释微丸释放速率的研究

 目的比较不同致孔剂及其用量对水难溶性药物布地奈德肠溶缓释微丸释药行为的影响。方法采用流化床空气悬浮包衣法制备载药丸芯,Surelease 缓释衣及Eudragit L30D-55肠溶衣制得布地奈德微丸。比较了缓释层中不同致孔剂及其用量对微丸释药速率的影响。结果布地奈德肠溶缓释微丸的释放速率随致孔剂的用量增加而加快,释药基本符合一级动力学模式,且药物释放速率常数与致孔剂用量成正比关系。相同用量的致孔剂对布地奈德释放的影响为Tween80,SDS>HPMC,Lactose>PVP>PEG400>PEG4000。结论不同致孔剂及其用量对布地奈德肠溶缓释微丸释放速率的影响较大,选择合适的致孔剂及其用量对获得适当的释药速率很重要。

Studies on Influence of Pore-Forming Agents on the Release Profile of Budesonide from Enteric-Coated Sustained Release Pellets

OBJECTIVE To compare the influence of different pore-forming agents and their amount on the release of budesonide enteric-coated sustained-release pellets.METHODS Budesonide pellets composed of drug loaded core,sustained-release layer and enteric-coated layer were prepared by air suspension method in the fluid bed.The influences of different pore-forming agents and their amount on the drug release were compared.RESULTS The drug release rate of budesonide pellets was increased significantly with the increasement of amount of pore-forming agents and the release behavior met the mode of first-order release process.There was a linear relationship between the amount of pore-forming agent and the release rate constant.The regulative ability of the different pore-forming agent in the study was as follows:Tween80,SDS>HPMC,Lactose>PVP>PEG400>PEG4000.CONCLUSION Different kinds of pore-forming agents and the amount used had significantly effects on the release of budesonide pellets.Proper release rate of the pellets can be obtained by using suitable pore-forming agent and its amount.