Department of Applied Chemistry, Faculty of Engineering, University of Miyazaki, 1-1 Gakuen Kibanadai Nishi, Miyazaki 889-2192, Japan.
Int J Pharm. 2013 Sep 10;453(2):587-93. doi: 10.1016/j.ijpharm.2013.05.058. Epub 2013 Jun 3.
Complex formation between indomethacin (Indo) and casein hydrolysate was developed as a novel technique for enhancing the water solubility of Indo. The complex (Indo-Pep) was prepared by mixing an ethanol solution of Indo and an aqueous solution of peptide mixture, followed by lyophilization. The water solubility of Indo-Pep under weakly acidic and neutral conditions is much higher than that of Indo alone. The water solubility of Indo increased with increasing quantity of peptide. Characterization of Indo-Pep using scanning electron microscopy, differential scanning calorimetry, and X-ray diffraction showed that Indo was incorporated in Indo-Pep in an amorphous state. The fluorescence quenching of Indo-Pep also suggested complexation between Indo and the peptides. An aqueous solution of Indo-Pep was fractioned by centrifugation followed by filtration using membrane filters and ultrafilters. Analysis of the fractions by dynamic light scattering and ultraviolet-visible spectroscopy showed that Indo-Pep consisted of small particles and was not a hydrocolloidal material.
将吲哚美辛（Indo）与酪蛋白水解物形成复合物，开发为一种提高吲哚美辛水溶性的新技术。将吲哚美辛的乙醇溶液与肽混合物的水溶液混合，然后冻干，制备复合物（Indo-Pep）。Indo-Pep 在弱酸性和中性条件下的水溶性远高于单独的 Indo。吲哚美辛的水溶性随肽量的增加而增加。使用扫描电子显微镜、差示扫描量热法和 X 射线衍射对 Indo-Pep 进行表征表明，吲哚美辛以无定形状态掺入 Indo-Pep 中。Indo-Pep 的荧光猝灭也表明了 Indo 与肽之间的络合。通过离心将 Indo-Pep 的水溶液分级，然后使用膜过滤器和超滤器过滤。对级分进行动态光散射和紫外可见光谱分析表明，Indo-Pep 由小颗粒组成，不是水胶体材料。
