ICGM, University Montpellier, CNRS, ENSCM, Montpellier, France.
IBMM, University Montpellier, CNRS, ENSCM, Montpellier, France.
AAPS PharmSciTech. 2020 Feb 24;21(3):94. doi: 10.1208/s12249-020-1633-3.
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 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® and Kollidon Cl®) 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.
本研究旨在探究褐藻酸的结构、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，对两批不同的褐藻酸进行了精确的表征（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 核磁共振、尺寸排阻色谱-多角度光散射、粘度、羧酸滴定、粉末流动性、真密度、激光粒度分析）。结果表明，分子量似乎会影响片剂的性质，分子量最低的褐藻酸可压性最差，弹性回复最低。此外，这些结果表明，将褐藻酸用作片剂配方中的填充赋形剂具有潜在的应用价值。最后，发现测试材料的崩解性能与商业超级崩解剂（Glycolys®和 Kollidon Cl®）相近，但与它们的溶胀力无关。这是首次得出结论，褐藻酸分子量的测定对于直接压片的应用非常重要，特别是对于获得具有可重现强度的片剂。
