Center of Clinical Pharmacology, The Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang, China.
Clin Transl Sci. 2024 May;17(5):e13819. doi: 10.1111/cts.13819.
The equivalence of absorption rates and extents between generic drugs and their reference formulations is crucial for ensuring therapeutic comparability. Bioequivalence (BE) studies are widely utilized and play a pivotal role in substantiating the approval and promotional efforts for generic drugs. Virtual BE simulation is a valuable tool for mitigating risks and guiding clinical BE studies, thereby minimizing redundant in vivo BE assessments. Herein, we successfully developed a physiologically based absorption model for virtual BE simulations, which precisely predicts the BE of the apixaban test and reference formulations. The modeling results confirm that the test and reference formulations were bioequivalent under both fasted and fed conditions, consistent with clinical studies. This highlights the efficacy of physiologically based absorption modeling as a powerful tool for formulation screening and can be adopted as a methodological and risk assessment strategy to detect potential clinical BE risks.
仿制药与其参比制剂之间的吸收速率和程度等效性对于确保治疗等效性至关重要。生物等效性（BE）研究被广泛应用，并在支持仿制药的批准和推广方面发挥着关键作用。虚拟 BE 模拟是一种降低风险和指导临床 BE 研究的有价值的工具，从而最大限度地减少体内 BE 评估的重复。在此，我们成功开发了一种用于虚拟 BE 模拟的基于生理学的吸收模型，该模型能够准确预测阿哌沙班测试和参比制剂的 BE。模型结果证实，在空腹和进食条件下，测试和参比制剂均具有生物等效性，与临床研究结果一致。这突出了基于生理学的吸收模型作为制剂筛选的有力工具的功效，可作为一种方法学和风险评估策略，用于检测潜在的临床 BE 风险。
