Compaction properties of crystalline pharmaceutical ingredients according to the Walker model and nanomechanical attributes
Compaction properties of crystalline pharmaceutical ingredients according to the Walker model and nanomechanical attributes
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DOI：
10.1016/j.ijpharm.2014.06.047
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发表时间：
2014-09-10
影响因子：
5.8
通讯作者：
Srcic, S.
中科院分区：
文献类型：
--
作者：
Egart, M.;Ilic, I.;Srcic, S.
本研究调查了所选活性成分（法莫替丁、硝苯地平、奥氮平、吡罗西康）的单晶力学性质对其体积压缩性和压缩性的影响程度。采用纳米压痕法测定了取向单晶的纳米力学属性，采用Walker和Heckel模型以及弹性松弛指数评估了取向单晶的体变形特性。体积和单晶塑性参数：沃克系数和压痕硬度之间建立了良好的相关性。Walker模型在评估所研究的api的整体变形特性方面显示出更大的实用价值，因为它们的特性与Heckel模型相比差异更明显。此外，由于建立了弹性松弛指数与柔度之间的相关性，因此可以在体水平上预测所研究材料的弹性性能。使用压痕硬度作为晶体原料药的价值也得到了证实，因为它们在体水平上的压实性能够被预测。机械互锁结构是大多数被研究的多晶形式的特征，导致单晶具有各向同性的力学性能。结果表明，在这种情况下，单个和整体力学性能之间的良好相关性是可以预期的。结果表明，晶体固有的变形特性在很大程度上决定了它们的压缩性和致密性。(C) 2014年Elsevier B.V.出版
This study investigates the extent to which single-crystal mechanical properties of selected active ingredients (famotidine, nifedipine, olanzapine, piroxicam) influence their bulk compressibility and compactibility. Nanomechanical attributes of oriented single crystals were determined with instrumented nanoindentation, and bulk deformational properties were assessed with the Walker and Heckel models as well as the elastic relaxation index. Good correlations were established between bulk and single-crystal plasticity parameters: the Walker coefficient and indentation hardness. The Walker model showed more practical value for evaluating bulk deformational properties of the APIs investigated because their properties differed more distinctly compared to the Heckel model. In addition, it was possible to predict the elastic properties of the materials investigated at the bulk level because a correlation between the elastic relaxation index and compliance was established. The value of using indentation hardness for crystalline APIs was also confirmed because their compactibility at the bulk level was able to be predicted. Mechanically interlocked structures were characteristic of most polymorphic forms investigated, resulting in single crystals having isotropic mechanical properties. It was revealed that in such cases good correlations between single and bulk mechanical properties can be expected. The results imply that innate crystal deformational properties define their compressibility and compactibility properties to a great extent. (C) 2014 Published by Elsevier B.V.