Structure-Properties Relationship in the Evaluation of Alginic Acid Functionality for Tableting
Structure-Properties Relationship in the Evaluation of Alginic Acid Functionality for Tableting
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DOI：
10.1208/s12249-020-1633-3
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发表时间：
2020-02-24
影响因子：
3.3
通讯作者：
Soulairol, Ian
中科院分区：
文献类型：
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作者：
Benabbas, Rihab;Sanchez-Ballester, Noelia M.;Soulairol, Ian
本研究的目的是研究海藻酸的结构、分子和颗粒特性与其在直接压片中的功能特性（可压片性、可压缩性、弹性、变形机制和崩解能力）之间的关系。因此，对两个不同批次的海藻酸进行了准确表征（X射线粉末衍射、傅里叶变换红外光谱、热重分析、扫描电子显微镜、H-1核磁共振、尺寸排阻色谱-多角度光散射、粘度测定、羧酸滴定、粉末流动性、真密度、激光粒度测定）。结果表明，分子量似乎影响片剂性质，并且具有最低分子量的海藻酸提供具有最低弹性恢复的最硬片剂。此外，这些结果显示了利用海藻酸作为片剂制剂中的填充赋形剂的潜在兴趣。最后，发现测试材料的崩解性能接近于商业超级崩解剂（Glycolys（R）和Kollidon Cl（R））的崩解性能，但与它们的溶胀力无关。可以得出结论，第一次，海藻酸分子量的测定似乎是直接压片应用的关键，特别是获得具有可重现强度的片剂。
The aim of this study is to investigate the relationship between the structural, molecular, and particulate properties of alginic acid and its functional characteristics in direct compression (tabletability, compressibility, elasticity, deformation mechanism, and disintegration ability). Therefore, accurate characterization of two different batches of alginic acid was executed (X-ray powder diffraction, Fourier-transform infrared spectroscopy, thermogravimetric analysis, scanning electronic microscopy, H-1 nuclear magnetic resonance, size exclusion chromatography - multi angle light scattering, viscosimetry, carboxylic acid titration, powder flowability, true density, laser granulometry). Results showed that molecular weight seems to affect tablet properties and that the alginic acid with the lowest molecular weight provides the hardest tablets with the lowest elastic recovery. Furthermore, these results show the potential interest of exploiting alginic acid as filler excipient in tablet formulation. Finally, disintegration properties of tested materials were found to be close to that of commercial superdisintegrants (Glycolys (R) and Kollidon Cl (R)) but not correlated to their swelling force. It can be concluded, for the first time, that the determination of alginic acid molecular weight seems key for applications in direct compression and in particular for obtaining tablets with reproducible strength.