采用有区分力的溶出曲线评价难溶性头孢菌素类仿制制剂的质量

The quality evaluation of insoluble cephalosporin generic preparations by discriminating dissolution curves

目的以难溶性头孢菌素类药物头孢克肟颗粒和头孢地尼胶囊为例,论证原料药pH-溶解度曲线与制剂在不同介质中溶出曲线的关系。方法以原料药的pH-溶解度曲线为依据,寻找具有区分力的溶出曲线,并使用有区分力的溶出方法评价仿制制剂的质量。结果头孢克肟颗粒具有区分力的溶出曲线为pH1.2溶出介质(60 min溶出度达到85%)和pH3.0溶出介质(120 min溶出度达到85%);头孢地尼胶囊具有区分力的溶出曲线介质为pH2.9溶出介质(60 min溶出度达到85%)。结论以具有区分力的多条溶出曲线研究参比制剂与仿制制剂的质量,有利于仿制药通过一致性评价。

Objective To demonstrate the relationship between pH-solubility curves of active pharmaceutical ingredient(API)and dissolution curves of preparations in different mediums by using insoluble cephalosporin,cefixime granules and cefdinir capsules as examples.Methods The discriminative dissolution curve was found according to pH-solubility of API.The quality of generic preparations was evaluated by discriminative dissolution curve.Results pH1.2dissolution medium(The dissolution rate of60min reached85%)and pH3.0dissolution medium(The dissolution rate of120min reached85%)were the discriminating dissolution curves of cefixime granules.pH2.9dissolution medium(The dissolution rate of60min reached85%)was the discriminative dissolution curve of cefdinir capsule.Conclusion The multiple discriminating dissolution curves are used to evaluate the quality of the reference preparation and the generic preparation,which is beneficial to the consistency evaluation of generic drugs.