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理解加巴喷丁片的变形行为和压缩速度效应。

Understanding Deformation Behavior and Compression Speed Effect in Gabapentin Compacts.

机构信息

Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Ave, Pittsburgh, PA 15282, USA.

Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Ave, Pittsburgh, PA 15282, USA.

出版信息

J Pharm Sci. 2021 May;110(5):2157-2166. doi: 10.1016/j.xphs.2020.12.021. Epub 2020 Dec 23.

DOI:10.1016/j.xphs.2020.12.021
PMID:33359044
Abstract

Deformation mechanism and strain rate sensitivity of gabapentin powder was investigated in this work. Heckel analysis, specific surface area and indentation hardness measurements revealed an intermediate yield pressure and brittle fracture as the dominant type of deformation mechanism during consolidation. Strain rate sensitivity of gabapentin was studied by compressing it at 1 mm/min and 500 mm/min compression speeds. Gabapentin demonstrated an atypical strain rate sensitivity in compactibility profile (tensile strength vs. solid fraction). Compacts of gabapentin compressed at fast speed showed an increase in tensile strength when compared with those compressed at slow speed. To understand the effect of compression speed on gabapentin's compactibility, PXRD analysis, surface area analysis, indentation hardness measurements, and consolidation modeling were performed. PXRD analysis carried out on compacts revealed no effect of speed on the physical solid-state stability of gabapentin. Specific surface area of compacts made at fast speed was higher than that of compacts made at slow speed. Indentation measurements performed on gabapentin compacts showed higher values of hardness in the case compacts made at fast speed. It was identified that at the fast compression speed, gabapentin shows greater particle fragmentation and form compacts with smaller pores.

摘要

本工作研究了普瑞巴林粉末的变形机制和应变速率敏感性。海克尔分析、比表面积和压痕硬度测量表明,在固结过程中,中间屈服压力和脆性断裂是主要的变形机制。通过在 1mm/min 和 500mm/min 的压缩速度下压缩普瑞巴林来研究其应变速率敏感性。普瑞巴林在可压缩性曲线(拉伸强度与固体分数)中表现出非典型的应变速率敏感性。与在低速下压缩的样品相比,在高速下压缩的普瑞巴林样品的拉伸强度增加。为了了解压缩速度对普瑞巴林可压缩性的影响,进行了粉末 X 射线衍射 (PXRD) 分析、比表面积分析、压痕硬度测量和固结建模。对压缩样品进行的 PXRD 分析表明,速度对普瑞巴林的物理固态稳定性没有影响。在高速下制备的压坯的比表面积高于在低速下制备的压坯。对普瑞巴林压坯进行的压痕测量显示,在高速压缩的情况下,硬度值较高。结果表明,在高速压缩下,普瑞巴林表现出更大的颗粒破碎,并形成具有更小孔的压坯。

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