水飞蓟宾葡甲胺缓释微丸的制备与体外释放度考察

Preparation and in vitro Release Behavior of Silybin N-Meglumine Sustained-release Pellet Capsules

目的制备水飞蓟宾葡甲胺缓释微丸,考察其体外释放度。方法采用离心造粒粉末层积法制备微晶纤维素空白丸芯。以收率及粒径分布为评价指标,考察载药微丸工艺。以Eudragit RS 30D/RL 30D水分散体混合物进行包衣,探讨包衣微丸的释药特征。结果水飞蓟宾葡甲胺缓释微丸的最佳处方与工艺条件为:黏合剂1%羟丙甲基纤维素(HPMC)溶液、黏度5 MPa·s,主机转速130 r·min-1,喷气压力0.3 MPa,浆泵转速6 r·min-1,抛光时间3 min,包衣增重7%,Eudragit RS/RL比例4∶1。体外释放接近一级释放模型,释药速度符合Fick's第一定律。结论离心造粒法制备水飞蓟宾葡甲胺缓释微丸工艺简单,具有缓释效果。

Objective To prepare silybin N-meglumine （SLB-M） sustained-release pellets capsules and study their release in vitro. Methods The microcrystalline cellulose （ MCC ） blank-pellets were prepared by means of powder layering with a centrifugal granulation equipment. The yield and size distribution were optimized as the main evaluation index. Then, Eudragit RL 30D/Eudragit RS 30D were used as the coating material to prepare SLB-M sustained-release pellets. The release properties of coated pellets was studied. Results The optimized formulation and procedure of SLB-M sustained-release pellets were as follows：taking 1% HPMC（5 cps） as adhesive, setting rotational speed of plate and pulp pump at 130 and 6 r ~ rain-~, respectively,atomization pressure as 0.3 MPa, sphronization for 3 min, the layer weight gains of Eudragit RL 30D/Eudragit RS 30D （ RS to RL,4 ＂ 1 ） being 7% of total weight. The in vitro release of the drug from pellets was in accordance with First-order kinetics model. Conclusion The technology of preparation is reliable and quality controllable, SLB-M sustained-release pellets prepared in this way show a significant sustained-release property.