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Ethylenediamine Salt Enhances the Solubility and Dissolution of Flurbiprofen

机译:乙二胺盐增强氟比洛芬的溶解度和溶解度

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摘要

Drugs that are poorly soluble in water are difficult to absorb orally, resulting in low bioavailability. Flurbiprofen (FLU) is an arylpropionic acid nonsteroidal anti‐inflammatory drug belonging to BCS class II, with low water solubility. In this study, a novel flurbiprofen‐ethylenediamine salt (FLU‐EDA) was successfully prepared via solvent crystallization. Its crystal structure was determined via single‐crystal X‐ray diffraction (SXRD). Further, the physicochemical properties of FLU‐EDA salt were characterized by powder X‐ray diffraction (PXRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT‐IR). The solubility and intrinsic dissolution rate (IDR) of FLU‐EDA salt in water were investigated. The results showed that compared with FLU, the solubility and IDR of FLU‐EDA salt increased by 57‐fold and 32‐fold, respectively. This indicates that FLU‐EDA salt can significantly enhance the solubility and dissolution rate of flurbiprofen in water. This study provides basic data and theory for the development of new formulations of flurbiprofen.
机译:难溶于水的药物难以口服吸收,导致生物利用度低。氟比洛芬 (FLU) 是一种芳基丙酸非甾体类抗炎药,属于 BCS II 类,水溶性低。在这项研究中,通过溶剂结晶成功制备了一种新型氟比洛芬-乙二胺盐 (FLU-EDA)。其晶体结构通过单晶 X 射线衍射 (SXRD) 确定。此外,通过粉末 X 射线衍射 (PXRD)、差示扫描量热法 (DSC) 和傅里叶变换红外光谱 (FT-IR) 对 FLU-EDA 盐的物理化学性质进行了表征。研究了 FLU-EDA 盐在水中的溶解度和内禀溶出率 (IDR)。结果表明,与 FLU 相比,FLU-EDA 盐的溶解度和 IDR 分别提高了 57 倍和 32 倍。这表明 FLU-EDA 盐可以显著提高氟比洛芬在水中的溶解度和溶解速率。本研究为氟比洛芬新制剂的开发提供了基础数据和理论。

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