摘要
目的:制备吲哚美辛(IMC)缓释微丸并考察其体外释放行为。方法:采用挤出滚圆法制备微丸,以微丸收率为考察指标,优选挤出速率、滚圆速度和滚圆时间参数水平;以体外释药曲线为考察指标,崩解剂微晶纤维素(MCC)、骨架材料羟丙甲基纤维素(HPMC)和润湿剂水的处方用量为因素,设计单因素试验筛选辅料处方,并进行处方验证试验及其释药机制研究。结果:优选的较佳工艺参数为挤出速度65r.min-1、滚圆速度650r.min-1、滚圆时间3min;优选的处方为MCC19、HPMC20、水6mL;验证试验表明所制得的IMC缓释微丸释放度重现性好且符合缓释制剂的要求,其释药机制为药物扩散和骨架溶蚀的混合型机制。结论:挤出滚圆法制备IMC缓释微丸方法可行,且制剂具有良好的体外缓释效果。
OBJECTIVE： To prepare Indomethacin sustained-release pellets and to investigate drug release behavior of it in vitro. METHODS： The pellets were prepared by extrusion-spheronization method. The extrusion velocity, spheronization velocity and spheronization time were optimized with the field of pellets as index. The formula of excipients was optimized by single-factor experiment with drug release curves as index and the amount of MCC, HPMC and water as factors. The validation test of formula was conducted and drug release behavior mechanism Was studied. RESULTS： The optimal technology parameters were as follows： extrusion velocity of 65 r·min^-1, spheronization velocity of 650 r·min^-1, spheronization time of 3 min. Optimal formula was as follows： MCC 19%, HPMC 20%, water 6 mL. Drug release behavior of prepared Indomethacin sustained-release pellets had good reproducibility and was up to requirement of sustained-release preparation, The drug release mechanism of pellet was drug diffusion and skeleton corrosion mechanism. CONCLUSIONS： The extrusion-spheronization method is feasible for the preparation of Indomethacin sustained-release pellets with sustained release characteristics.
出处
《中国药房》
CAS
CSCD
北大核心
2011年第17期1583-1586,共4页
China Pharmacy
基金
重庆市自然科学基金项目(2009BB5106)
重庆高校优秀成果转化资助项目(KJ08B06)
西南大学博士基金项目(SWUB2008032)
关键词
吲哚美辛
挤出滚圆法
缓释微丸
制备
工艺参数
释药机制
Indomethacin
Extrusion-spheronization method
Sustained-release pellet
Preparation
Technology parameters
Drug release mechanism
