Effects of roll mixing with beta-cyclodextrin on enhancing solubilities of water insoluble drugs.
Effects of roll mixing with beta-cyclodextrin on enhancing solubilities of water insoluble drugs.
复制标题
β-环糊精滚动混合对提高水不溶性药物溶解度的影响。
DOI：
--
复制
发表时间：
1989
期刊：
影响因子：
--
通讯作者：
A. Yamamoto
中科院分区：
文献类型：
--
作者：
Y. Nozawa;A. Yamamoto
为了通过使用与β-环糊精（CyD）的滚混来增加水不溶性药物的溶解度，与如与水捏合和物理混合的不同混合系统的平衡浓度进行比较，检查了10种药物吲哚美辛、灰黄霉素、硝苯地平等的平衡浓度。药物在滚动混合系统中的平衡浓度比除醋酸可的松（CA）系统外的其他系统更有利，并且与除吉他霉素之外的药物的溶解度相比，它明显增加。几乎所有的药物都是结晶状态，很容易通过与CyD的辊混过程变成无定形形式。在相对湿度（RH）为97%的增湿环境中暴露24小时后，X射线衍射图谱显示，与CA或己烯雌酚（DB）混合的无定形产品卷由于CyD的包合物而转变为结晶形式。另一个辊混合的产物表现出水合CyD的结晶图案。预计混药卷溶解度的明显增加与包合物的形成或药物与CyD之间的某些分子相互作用有关，这是基于IR光谱上吸收带的轻微变化。
To increase a solubility of water insoluble drugs by the use of roll mixing with beta-cyclodextrin (CyD), equilibrium concentrations of ten medicinal drugs indomethacin, griseofulvin, nifedipine and so on were examined in comparison with those of different mixed systems as kneading with water and physical mixing. The equilibrium concentration of drug in the roll mixed systems was more advantageous than the others excluding the systems of cortisone acetate (CA), and it increased apparently as compared to the solubility of the drugs except for kitasamycin. Almost all of drugs being a crystalline state turned readily to an amorphous form by the procedures of roll mixing with CyD. The amorphous product roll mixed with CA or diethylstilbestrol (DB) changed to the crystalline form due to the inclusion complexes of CyD in X-ray diffraction patterns, when these were exposed on humidifing atmospheres of relative humidity (RH) 97% for 24 hours. The another roll mixed products exhibited the crystalline pattern of the hydrated CyD. Apparent increases in the solubility of drug roll mixed were expected to relate a formation of inclusion compounds or certain molecular interactions between the drug and CyD, which was based upon slight changes in absorption bands on IR spectra.