Department of Material and Analytical Sciences, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.
Department of Material and Analytical Sciences, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.
J Pharm Sci. 2021 Jun;110(6):2570-2574. doi: 10.1016/j.xphs.2021.03.010. Epub 2021 Mar 18.
The evolution of tablet strength is mainly influenced by deformability (bonding area) and strength of intermolecular interactions (bonding strength) from the intrinsic material properties and tableting process, respectively. Therefore, understanding of intrinsic material attributes is important for in-silico drug product designs. The present study shows that the separate effect of the above two factors can be better understood by systematic evaluation of pure APIs and their formulations. Using tensile strength, elastic modulus and yield stress as critical material attributes, a proof of concept shown in this work emphasizes that materials with greater deformability tend to possess greater tensile strength at comparable bonding strengths. In contrast, the influence of the deformability parameter is hidden when formulations are used, leading to a scenario where the effects of bonding area and bonding strength are more inseparable.
片剂强度的演变主要受到内在材料特性和压片工艺的可变形性(结合面积)和分子间相互作用强度(结合强度)的影响。因此,了解内在材料属性对于虚拟药物产品设计很重要。本研究表明,通过对纯 API 及其制剂进行系统评估,可以更好地理解上述两个因素的单独影响。本文使用拉伸强度、弹性模量和屈服应力作为关键材料属性,展示了一个概念验证,强调了在可比结合强度下,具有较大可变形性的材料往往具有较大的拉伸强度。相比之下,当使用制剂时,变形参数的影响被隐藏,导致结合面积和结合强度的影响更加不可分割。