Tozuka Yuichi, Oguchi Toshio, Yamamoto Keiji
Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoicho, Inage-ku, Chiba 263-8522, Japan.
Pharm Res. 2003 Jun;20(6):926-30. doi: 10.1023/a:1023851622676.
The aim of this study was to estimate the molecular state of salicylamide on the surface of mesoporous silicas and to investigate the dissolution behavior of salicylamide from the solid dispersion.
Folded sheets mesoporous material (FSM-16) were used as a porous material. The molecular state of salicylamide was estimated by powder X-ray diffractometry, infrared spectroscopy, and fluorescence spectroscopy.
The molecular state of salicylamide can be changed by simple blending with FSM-16. When a physical mixture of 25% salicylamide and 75% FSM-16 was heated at 120 degrees C for 3 h, amorphization of salicylamide was observed from the powder X-ray diffraction pattern. The fluorescence emission peak of salicylamide at 433.5 nm shifted to a longer wavelength of 447.5 nm after heating. Changes in fluorescence decay curve suggested that salicylamide molecules were dispersed into the hexagonal FSM-16 channels during the heating process. Enhanced dissolution in the initial stage of salicylamide from the sealed heated sample was observed in comparison with salicylamide crystals.
Heat treatment of a physical mixture of salicylamide with FSM-16 gave a solid dispersion in which the salicylamide molecules changed to an amorphous state by adsorption onto the FSM-16 channels. Amorphization of salicylamide contributed to the improvement of dissolution.
本研究旨在评估水杨酸酰胺在介孔二氧化硅表面的分子状态，并研究水杨酸酰胺从固体分散体中的溶解行为。
采用折叠片层介孔材料（FSM-16）作为多孔材料。通过粉末X射线衍射、红外光谱和荧光光谱评估水杨酸酰胺的分子状态。
水杨酸酰胺的分子状态可通过与FSM-16简单混合而改变。当25%水杨酸酰胺和75% FSM-16的物理混合物在120℃加热3小时时，从粉末X射线衍射图谱中观察到水杨酸酰胺的非晶化。加热后，水杨酸酰胺在433.5nm处的荧光发射峰移至447.5nm的更长波长处。荧光衰减曲线的变化表明，在加热过程中水杨酸酰胺分子分散到六方FSM-16通道中。与水杨酸酰胺晶体相比，观察到密封加热样品中的水杨酸酰胺在初始阶段的溶解增强。
水杨酸酰胺与FSM-16的物理混合物经热处理得到一种固体分散体，其中水杨酸酰胺分子通过吸附到FSM-16通道上而转变为无定形状态。水杨酸酰胺的非晶化有助于溶解的改善。
