头孢妥仑匹酯片溶出度一致性评价的方法学研究

Methodological study on the consistency evaluation of dissolution of cefditoren pivoxil tablets

目的通过不同的溶出条件选择处方使自制样品与原研参比制剂有相同的体外溶出度。方法通过美国食品药品监督管理局非模型依赖法的(f_(2))相似因子对头孢妥仑匹酯片的溶解性能进行研究。用氯化钠-盐酸混合液作为溶出液,体积900mL,用桨法,转速50r·min^(-1),按紫外-可见分光光度法,波长为272nm进行检测,并对自制头孢妥仑匹酯片与参比制剂的溶出性能进行对比,确定其溶出度性能和影响因素。结果头孢妥仑匹酯在7.5~22.5μg·mL^(-1)内,线性关系好,标准曲线为A=3.25×10^(-2)C-1.80×10^(-2)(R^(2)=0.9997),平均回收率为99.33%。在体外实验中,自制样品与参比制剂的溶出度相似因子f_(2)值差异很小,且符合预期。结论头孢妥仑匹酯片的溶出度检查方法适用于本制剂的研制,通过比较相似因子选择出来的处方制剂能大幅提高生物等效性的成功率。

Objective To select a prescription through different dissolution conditions to ensure that the self-made sample has the same in vitro dissolution as the original reference formulation.Methods We investigated the dissolution performance of cefditoren pivoxil tablets using the(f2)similarity factor of the US Food and Drug Administration non model dependent method.A sodium chloride hydrochloric acid mixture was used as the dissolution solution,with a volume of 900 mL.The paddle method was used,rotating speed 50 r·min(-1),and UV-visible spectrophotometer was used,The measurement wavelength was 272 nm.Finally,we compared the dissolution performance of self-made cefditoren pivoxil tablets with the reference formulation,and determined their dissolution performance and corresponding influencing factors.ResultsThe curve equation for ceftriaxone is A=3.25×10^(-2) C-1.80×10^(-2)(R^(2)=0.9997),with a linear range of 7.5-22.5μg·mL^(-1),with an average recovery rate of 99.33%.Through the dissolution testing method used,we found that in the in vitro experiment,the difference in dissolution similarity factor of f_(2),between the self-made sample and the reference formulation we used was very small and met expectations.Conclusion The dissolution test method for cefditoren pivoxil tablets is suitable for the development of this formulation.Prescription formulations selected by comparing similar factors can significantly improve the success rate of bioequivalence.