Knapik-Kowalczuk Justyna, Kramarczyk Daniel, Chmiel Krzysztof, Romanova Jana, Kawakami Kohsaku, Paluch Marian
Faculty of Science and Technology, Institute of Physics, University of Silesia, SMCEBI, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland.
International Center for Materials Nanoarchitectonics, National Institute for Materials Science, Tsukuba, Ibaraki 305-0044, Japan.
Pharmaceutics. 2020 Apr 22;12(4):384. doi: 10.3390/pharmaceutics12040384.
In this paper, the role of mesoporous silica (MS) particle size in the stabilization of amorphous simvastatin (SVT) is revealed. For inhibiting recrystallization of the supercooled drug, the two MS materials (Syloid XDP 3050 and Syloid 244 FP) were employed. The crystallization tendency of SVT alone and in mixture with the MS materials was investigated by Differential Scanning Calorimetry (DSC) and Broadband Dielectric Spectroscopy (BDS). Neither confinement of the SVT molecules inside the MS pores nor molecular interactions between functional groups of the SVT molecules and the surface of the stabilizing excipient could explain the observed stabilization effect. The stabilization effect might be correlated with diffusion length of the SVT molecules in the MS materials that depended on the particle size. Moreover, MS materials possessing different particle sizes could offer free spaces with different sizes, which might influence crystal growth of SVT. All of these factors must be considered when mesoporous materials are used for stabilizing pharmaceutical glasses.
本文揭示了介孔二氧化硅（MS）粒径在无定形辛伐他汀（SVT）稳定化过程中的作用。为抑制过冷药物的重结晶，使用了两种MS材料（Syloid XDP 3050和Syloid 244 FP）。通过差示扫描量热法（DSC）和宽带介电谱（BDS）研究了单独的SVT以及与MS材料混合后的结晶趋势。SVT分子在MS孔内的受限情况以及SVT分子官能团与稳定化辅料表面之间的分子相互作用，均无法解释所观察到的稳定化效果。稳定化效果可能与SVT分子在MS材料中的扩散长度相关，而扩散长度取决于粒径。此外，具有不同粒径的MS材料可提供不同尺寸的自由空间，这可能会影响SVT的晶体生长。在将介孔材料用于稳定药物玻璃态时，所有这些因素都必须加以考虑。
