Tozuka Yuichi, Wongmekiat Arpansiree, Kimura Kyoko, Moribe Kunikazu, Yamamura Shigeo, Yamamoto Keiji
Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan.
Chem Pharm Bull (Tokyo). 2005 Aug;53(8):974-7. doi: 10.1248/cpb.53.974.
The interaction between FSM-16 and flurbiprofen (FBP) in the mesopores of FSM-16 was investigated by using three types of FSM-16 with different pore diameters, i.e., FSM-16(Oc), FSM-16(Do) and FSM-16(Doc) (pore diameters 16.0, 21.6, 45.0 A, respectively). Solid dispersions of 30% FBP-70% FSM-16 were prepared by solvent evaporation and sealed-heating of the physical mixture at 100 degrees C for 6 h. Changes in the molecular state of FBP were investigated using powder X-ray diffractometry, thermal analysis and FT-IR spectroscopy. The changes in pore diameter and specific surface area of FSM-16 systems were investigated by small angle X-ray scattering and nitrogen gas adsorption. Powder X-ray diffractometry and thermal analysis revealed that FBP was adsorbed onto the mesopores of FSM-16(Do) and FSM-16(Doc), leading to an amorphous state, while no change was observed for FSM-16(Oc). Fourier-transformed IR spectroscopy showed a hydrogen bond interaction between the carbonyl groups of FBP and the silanol groups of FSM-16. The pore diameter and specific surface area of FSM-16 in solid dispersions decreased due to the adsorption of FBP. Improved dissolution of FBP from solid dispersions prepared by the evaporation and the sealed-heating methods was observed in comparison with FBP crystals.
通过使用三种不同孔径的FSM-16，即FSM-16（Oc）、FSM-16（Do）和FSM-16（Doc）（孔径分别为16.0、21.6、45.0 Å），研究了FSM-16中FSM-16与氟比洛芬（FBP）在介孔中的相互作用。通过溶剂蒸发和将物理混合物在100℃密封加热6小时制备了30% FBP-70% FSM-16的固体分散体。使用粉末X射线衍射、热分析和傅里叶变换红外光谱研究了FBP分子状态的变化。通过小角X射线散射和氮气吸附研究了FSM-16体系孔径和比表面积的变化。粉末X射线衍射和热分析表明，FBP吸附在FSM-16（Do）和FSM-16（Doc）的介孔上，导致无定形状态，而FSM-16（Oc）未观察到变化。傅里叶变换红外光谱显示FBP的羰基与FSM-16的硅醇基之间存在氢键相互作用。由于FBP的吸附，固体分散体中FSM-16的孔径和比表面积减小。与FBP晶体相比，观察到通过蒸发和密封加热方法制备的固体分散体中FBP的溶出度提高。
