Pharmaceutical Properties of the Phloretin–4,4′-Bipyridine Cocrystal: Structure Analysis, Drug Release Profile, and Antioxidant Activity Research

作者：Zhongyu Lu, Gengzhen Yao, Huanglie Xie, Dawei Wang, Yanfen Chen, Wei Zhu · 发表于：ACS Omega · 年份：2024 · DOI：10.1021/acsomega.4c01136 · 被引用次数：5 · 研究领域：Crystallography and molecular interactions、Crystallization and Solubility Studies、Chemical and Physical Properties in Aqueous Solutions

High Resolution Image Download MS PowerPoint Slide To improve the water solubility of phloretin, we synthesized the Phl–4B cocrystal using the solvent evaporation method. Various analytical techniques including powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), 1 HNMR, and single-crystal X-ray diffraction (SCXRD) were employed to evaluate the crystal thermodynamics and structure. The results of PXRD and SCXRD showed that it was a new cocrystal crystallized in the P -1 space group of the triclinic system. Thermal analysis confirmed the purity of the Phl–4B cocrystal. The equilibrium solubility of the Phl–4B cocrystal in pH 1.2 was improved. In vitro simulated digestion experiments indicated that the release of the Phl–4B cocrystal followed Fick diffusion. The stability activity of phloretin after pharmaceutical cocrystallization was improved. The antioxidant of the Phl–4B cocrystal was better than that of pure Phl.