磷酸卡维地洛缓释微丸的制备及生物等效性研究

Preparation and biological equivalence study of Carvedilol phosphate sustained-release pellets

目的制备与参比制剂生物等效的磷酸卡维地洛缓释微丸。方法采用流化床制备磷酸卡维地洛载药微丸,进一步制备缓释微丸,采用正交实验优化处方工艺。结果载药微丸的最佳处方为:丸芯粒径0.35~0.5 mm,崩解剂用量15%,黏合剂用量10%,增溶剂用量15%;缓释微丸的最佳处方为:包衣增重7%,包衣液浓度50%,致孔剂用量5%,二氧化硅用量10%。结论自研制剂与参比制剂生物等效。

OBJECTIVE To prepare Carvediiol phosphate sustained - release pellets and to study the biological equivalence. METHODS A fluidized bed was used to prepare drug - layered pellets and sustained - release pellets. The orthogonal experiment was used to optimize the prescription process. RESULTS The formulation of Carvedilol phosphate drug - layered pellets is as follows： Pellets diameter of 0.35 -0.5 mm, disintegrating agent of 15%, binder of 10% and solubilizer of solvent of 15%. The prescription of carvedilol phosphate sustained - release pellets is as follows ： Coating weight of 7 %, coating liquid concentration of 50%, porogen of 5 % and silica dioxide of 10%. CONCLUSION The biological equivalence of the developed formulation and the marked product are consistent.