熔融法制备5-单硝酸异山梨酯缓释微丸及其体外释放考察  

Preparation of 5-isosorbide mononitrate sustained-release pellets by melt agglomeration and its release behaviors in vitro

作　　者：刘春憬 

机构地区：[1]青岛科技大学药学院,山东青岛266042

出　　处：《中南药学》2015年第1期28-30,共3页Central South Pharmacy

摘　　要：目的制备5-单硝酸异山梨酯缓释微丸,并对其体外释放度进行考察。方法采用高速熔融搅拌法制备5-单硝酸异山梨酯微丸,以微丸体外溶出参数t50为考察指标设计正交试验对处方进行筛选,通过释放度曲线药物代谢动力学拟合确定微丸的缓释机制。结果确定的最佳处方为每粒胶囊含有主药60 mg、预胶化淀粉16 mg、固体石蜡100 mg、单硬脂酸甘油酯16 mg、磷酸氢钙120 mg、硫酸钙适量;所制备的5-单硝酸异山梨酯缓释微丸的体外释放行为符合Higuchi方程Qt=0.242 2t1/2+0.084 2(r=0.996 0)。结论采用高速熔融搅拌法制备的5-单硝酸异山梨酯缓释微丸表面光滑,圆整度高,具有良好的缓释效果。Objective To prepare 5-isosorbide mononitrate sustained-rel ease pellets and study its in vitro drug release. Methods Drug-contained pellets were prepared by the melt pelletization in a high-speed mixer, the orthogonal design was used to optimize the prescription with the pellets, in vitro solubility parameter t50 was used as the indicator, and the mechanism of drug releasing from pellets was studied. Results The best prescription was determined as each capsule containing 60 mg main drug, 16 mg pregelatinized starch, 100 mg paraffin wax, 16 mg glycerol monostearate, 120 mg calcium hydrogen phosphate, and an appropriate amount of calcium sulfate. The release of the drug from sustained-release pellets fit the Higuchi equation： Qt=0.242 2t1/2＋0.084 2（r = 0.996 0）. Conclusion The 5-isosorbide mononitrate sustained-release pellets made by this technique have smooth surface, high roundness and a fairly good sustained-release profile.

关 键 词：5-单硝酸异山梨酯 熔融法 缓释微丸 体外释放 

分 类 号：R94[医药卫生—药剂学]