化学药物口服缓控释制剂体内外相关性研究(5)

ChineseJournalofNewDrugs2010,19(10)

情况下,偏差浮动可适当放宽至25%以内;如超过

25%的限度,则可能影响到产品的体内行为,建议进行生物等效性试验,验证上下限之间生物等效。根据 口服缓释制剂:体内外相关性的创建、评价和应用 ,拥有IVIVC模型后可能会允许设定较宽的释放度质量标准,其取决于IVIVC模型的预测能力(即,采用卷积分或其他适当的建模计算方法绘制血药浓度 时间曲线,并确定在试验中,比较采用释放度标准所能允许的最快和最慢释放速率的批次分别预测得到的Cmax和AUC,两者的最大差异是否不超过20%)。

4 小结

按我国目前的药品注册法规要求,在开发口服缓控释制剂时,如果仍按照凭经验的研发模式,风险必然加大,因此必须引入新的思路和方法,以适应当前的药品注册要求。IVIVC作为一种预测模型,能够在优化处方工艺、辅助设定体外释放度质量标准和支持生物等效性豁免方面发挥重要作用,有助于降低研发口服缓控释制剂的风险,节省研发成本和

注册时间,希望我国药品研发者和注册申请人重视

IVIVC并积极开展相关研究工作。

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