Otsuka M, Matsuda Y
Kobe Pharmaceutical University, Japan.
J Pharm Sci. 1995 Dec;84(12):1434-7. doi: 10.1002/jps.2600841209.
The physicochemical properties of phenytoin (PHT) combined with various kinds of surfactants at 40 w/w % such as sodium lauryl sulfate (SLS), sodium deoxycholate (DCNa), and the sucrose ester of stearic acid (SE) by a cogrinding method were investigated by X-ray diffraction analysis, Fourier transformed infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and dissolution kinetics in 2nd fluid (Japanese Pharmacopoeia XII, pH 6.8, 37 degrees C). All X-ray diffraction peak intensities of the coground mixtures were decreased by grinding, and the product with DCNa grinding for 3 h transformed into a noncrystalline solid, but the products with SE and SLS were not. The solubilities of ground products with SLS and SE were almost the same as those of respective physical mixtures. However, the apparent solubility of ground products with DCNa was 28.7 times higher than that of the physical mixture.
采用共研磨法,在40 w/w%的条件下,研究了苯妥英(PHT)与各种表面活性剂(如十二烷基硫酸钠(SLS)、脱氧胆酸钠(DCNa)和硬脂酸蔗糖酯(SE))结合后的物理化学性质,通过X射线衍射分析、傅里叶变换红外(FT-IR)光谱、差示扫描量热法(DSC)以及在第二液(日本药典 XII,pH 6.8,37℃)中的溶解动力学进行研究。共研磨混合物的所有X射线衍射峰强度通过研磨而降低,用DCNa研磨3小时的产物转变为非晶态固体,但用SE和SLS研磨的产物则没有。用SLS和SE研磨产物的溶解度与各自物理混合物的溶解度几乎相同。然而,用DCNa研磨产物的表观溶解度比物理混合物高28.7倍。