Liu Jinwen, Li Yongji, Ao Wuliji, Xiao Yingge, Bai Meirong, Li Shuyan
College of Traditional Mongolian Medicine, Inner Mongolia Minzu University, Tongliao 028000, China.
School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin 150040, China.
ACS Omega. 2022 Oct 24;7(44):39907-39912. doi: 10.1021/acsomega.2c04021. eCollection 2022 Nov 8.
This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD increased by five times compared with aprepitant. In addition, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC) results suggested the presence of amorphous-form aprepitant inside SD. According to Fourier transform infrared (FTIR) spectroscopy, intermolecular hydrogen bonds were detected between polymer and aprepitant. The Caco-2 cell experiment proved that SD did not lower the transepithelial electrical resistance (TEER) values but improved the permeation amount of aprepitant. Additionally, the SD of aprepitant displayed excellent stability.
本研究聚焦于通过制备固体分散体（SD）来改善水溶性差的阿瑞匹坦的理化特性。为了用低取代羟丙基甲基纤维素琥珀酸酯（HPMCAS-LF）制备固体分散体，采用了溶剂蒸发法。基于溶出度分析，固体分散体的溶出速率与阿瑞匹坦相比提高了五倍。此外，扫描电子显微镜（SEM）、X射线粉末衍射（XRPD）和差示扫描量热法（DSC）结果表明固体分散体内存在无定形阿瑞匹坦。根据傅里叶变换红外（FTIR）光谱，检测到聚合物与阿瑞匹坦之间存在分子间氢键。Caco-2细胞实验证明，固体分散体不会降低跨上皮电阻（TEER）值，但提高了阿瑞匹坦的渗透量。此外，阿瑞匹坦固体分散体表现出优异的稳定性。
