磷酸特地唑胺片的处方工艺及体外溶出行为的研究

Research on the formulation, the preparation technology and the in vitro dissolution behavior of tedizolid phosphate tablets

目的对磷酸特地唑胺片的处方及工艺进行研究,制备磷酸特地唑胺片,并对其体外溶出行为进行研究。方法参照国外上市片"SIBEXTRO"的处方及体外释放行为,对黏合剂、崩解剂、填充剂及包衣增重进行研究,筛选出合理的处方工艺,并对其进行放大。结果最终确定处方工艺为磷酸特地唑胺:200mg,甘露醇:110mg,微晶纤维素:60mg;聚维酮K30:6mg;交联聚维酮:12mg(内加),8mg(外加);硬脂酸镁:4mg;薄膜包衣预混剂:12mg;以纯化水为黏合剂。结论确定了处方工艺的稳定性,适合放大生产,体外溶出行为与市售品相似,处方工艺设计合理。

Objective To study the formulation, the preparation technology and the in vitro dissolution behavior of tedizolid phosphate tablets. Methods According to the formulation and in vitro dissolution behavior of ＂SIBEXTRO＂ on foreign markets, experiments were carried out on its binders, disintegrating agents, diluents and coating weights. A reasonable formulation and the preparation technology was screened and large scale production was taken out. Results The formulation was ultimately determined including 200mg of tedizolid phosphate, 120mg of mannitol, 50mg of microcrystalline cellulose, 6mg povidone, 12mg（inside） of crospovidone, 8mg（outside） of crospovidone, 4mg of magnesium stearate, 12mg of pelIicle coating pre-mixing agent, and purified water as a binder. Conclusion The formulation and the preparation technology determined is stable and suitable for the amplification production. The in vitro dissolution behavior of the corresponding tablets is similar to that of the commercial products.