盐酸地尔硫卓缓释脉冲微丸胶囊的体外释放研究

STUDY ON THE PREPARATION OF SUSTAINED-RELEASE AND PULSATILE PELLETS OF DILTIAZEM HYDROCHLORIDE

目的:制备盐酸地尔硫卓缓释脉冲控释微丸胶囊。方法:采用丙烯酸树脂Ⅱ号和微晶纤维素(MCC)为骨架材料制备盐酸地尔硫卓缓释微丸;采用低取代羟丙基纤维素(Low Substituted Hydroxypropylcellulose L-HPC)为内层溶胀材料,选用乙基纤维素水分散体(Surelease)为外层控释材料制备脉冲微丸。将两种微丸混合后制成缓释脉冲微丸胶囊,同时考察体外溶出度的影响因素。结果:体外释放试验证明,缓释微丸体外12h可持续释12h,脉冲微丸体外可达到时滞为4h,滞后1.5 h,累积释药80%以上的脉冲释药效果。两种微丸按比例混合后,其释药机制符合一级释药模型,达到良好的混合释放效果。结论:该制剂具有良好的缓释与脉冲效果。

Objective：To study the preparation of sustained-release and pulsatile pelletsof Diltiazem Hydrochloride （ DIL ） . Methods：To preparation sustained-release solid dispersion of DIL with acrylic resinIIand MCC;The cores of pulstile pellets were prepared by extrusion-spheronization and coated with low-substitued hydroxypropylcellulose （ L-HPC ） as the inner swelling layer and ethylcellulose aqueous dispersion （ Surelease ） as the outer controlled layer. The two kinds of pellets mixed to preparation Sustained-release and Pulsatile Pellets. Results：The sustained-release pellets can release to 12h;The pulstile release pellets,with a lag time of 4h and more than 80% released within following 1. 5h under the simulated gastro-intestinal pH conditons. To mixed two kinds of pelltes can meet the requirements of preparation. Conclusion：The pellets have an ideal sustained-release and pulsatile release.