熔融高速搅拌法制备双氯芬酸钠缓释胶囊的研究

Studies on Preparation of Diclofenac Sodium Sustained-release Capsules by High-shear Melt Agglomeration

目的研究熔融高速搅拌法制备双氯芬酸钠缓释胶囊及其体外释药行为。方法采用KJZ-10型熔融高速搅拌制粒机制备含药微丸,以微丸体外释放度为指标,考察处方工艺因素对微丸体外释放度的影响,通过释放度曲线药动力学拟合确定微丸缓释机制。结果双氯芬酸钠微丸体外释放行为符合Higuchi方程Y=35.43t1/2-16.1523(r=0.9988),释药机制主要是骨架溶蚀和扩散释放。结论该技术制备的双氯芬酸钠缓释微丸具有较好的释药性能及良好的缓释效果。

OBJECTIVE To prepare diclofenac sodium sustained-release pellets by high-shear melt agglomeration technology and study its in vitro drug release. METHODS Drug-contained pellets were prepared in a high-shear granulator, and the influencing factors of formulation and technique on pellets releasing profile were investigated and the mechanism of drug releasing from pellets was also studied. RESULTS The release of the drug from pellet was in accordance with Higuchi equation： Y=35.43t1/2-16.152 3（r=0.998 8）. The mechanism of diclofenac sodium releasing from pellets was matrix erosion and diffusion. CONCLUSION The diclofenac sodium sustained-release pellets made by this technique provided a rather good sustained-release profile.