Otsuka Yuta, Utsunomiya Yuiko, Umeda Daiki, Yonemochi Etsuo, Kawano Yayoi, Hanawa Takehisa
Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Research Institute for Science and Technology, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Pharmaceuticals (Basel). 2020 Jul 10;13(7):147. doi: 10.3390/ph13070147.
This study aimed to investigate the effect of polymers and storage relative humidity on amorphous rebamipide (RB) and its solid dispersion phase transformation using chemometrics based on multiple datasets. The amorphous RB was prepared using particle mixture and grinding methods with hydroxypropyl cellulose, polyvinylpyrrolidone, and sodium dodecyl sulfate. Prepared amorphous RB and solid dispersion samples were stored under a relative humidity of 30% and 75% for four weeks. Infrared spectra of the dispersion samples suggested that the hydrogen bond network was constructed among quinolinone, carbonyl acid, and amide of RB and other polymers. The dataset combining near-infrared (NIR) spectra and powder X-ray diffractograms were applied to principal component analysis (PCA). The relationship between diffractograms and NIR spectra was evaluated using loadings and the PCA score. The multiple spectra analysis is useful for evaluating model amorphous active pharmaceutical ingredients without a standard sample.
本研究旨在基于多个数据集，运用化学计量学方法研究聚合物和储存相对湿度对无定形瑞巴派特（RB）及其固体分散体相变的影响。采用颗粒混合法和研磨法，以羟丙基纤维素、聚乙烯吡咯烷酮和十二烷基硫酸钠制备无定形RB。将制备好的无定形RB和固体分散体样品在30%和75%的相对湿度下储存四周。分散体样品的红外光谱表明，RB的喹啉酮、羰基酸和酰胺与其他聚合物之间构建了氢键网络。将近红外（NIR）光谱和粉末X射线衍射图相结合的数据集应用于主成分分析（PCA）。使用载荷和PCA得分评估衍射图与NIR光谱之间的关系。多重光谱分析对于在没有标准样品的情况下评估模型无定形活性药物成分很有用。
