格列美脲片溶出度测定及对其体内外相关性考察

Dissolution Testing of Glimepiride Tablets and Evaluation of in Vivo-in Vitro Correlation

目的建立格列美脲片体内外相关的溶出度测定方法。方法采用桨法及流通池法,进行体外溶出试验,计算平均累积溶出度,并与体内吸收分数线性拟合;用相似因子(f2)评价7个厂家格列美脲片溶出度曲线的相似性。结果传统溶出方法测定格列美脲片在p H6.8条件下区分度较强,但体内外相关性较差;建立的流通池测定体外累积溶出量与体内吸收分数具有显著的相关性,回归方程为Fa=0.580 8 Fb+27.753 5(R^(2)=0.995 0)。7个厂家生产的格列美脲片,除B、D及本土化制剂外,其余均与原研不相似。结论所建立的格列美脲片溶出度测定方法具有良好的体内外相关性,可以用于控制其质量。

OBJECTIVE To develop a dissolution method for the glimepiride tablets of in vivo-in vitro correlation. METHODS The dissolution tests in vitro were carried out by using the slurry method and the flowing-through cell method. The average cumulative dissolutions were calculated and fitted with the absorption fraction in vivo,and the dissolution curves for glimepiride tablets of seven manu factures were evaluated by f2. RESULTS Under the condition of p H6.8,the traditional dissolution method for the determination of glimepiride tablets had a strong discrimination,but a poor in vivo-in vitro correlation. The cumulative dissolutions in vitro and absorption fraction in vivo had a significant correlation by the flowing-through cell method with the regression equation was 0.580 8 Fb+27.753 5( R^(2)= 0.995 0).The glimepiride tablets produced by seven manu factures,except for B,D and the localization,had no correlation with the original developer. CONCLUSION The dissolution determination method of glimepiride tablets has a good in vivo-in vitro correlation,and can be used to control its quality.