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Pharmaceutical Properties of the Phloretin–4,4′-Bipyridine Cocrystal: Structure Analysis, Drug Release Profile, and Antioxidant Activity Research
ACS Omega ( IF 3.7 ) Pub Date : 2024-07-08 , DOI: 10.1021/acsomega.4c01136 Zhongyu Lu 1 , Gengzhen Yao 1 , Huanglie Xie 1 , Dawei Wang 2 , Yanfen Chen 1 , Wei Zhu 3
ACS Omega ( IF 3.7 ) Pub Date : 2024-07-08 , DOI: 10.1021/acsomega.4c01136 Zhongyu Lu 1 , Gengzhen Yao 1 , Huanglie Xie 1 , Dawei Wang 2 , Yanfen Chen 1 , Wei Zhu 3
Affiliation
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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), 1HNMR, 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.
中文翻译：
根皮素–4,4′-联吡啶共晶的药物特性：结构分析、药物释放曲线和抗氧化活性研究
为了提高根皮素的水溶性，我们采用溶剂蒸发法合成了Phl-4B共晶。采用各种分析技术，包括粉末 X 射线衍射 (PXRD)、热重分析 (TGA)、差示扫描量热法 (DSC)、傅里叶变换红外 (FTIR)、 1 HNMR 和单晶 X 射线衍射 (SCXRD)评估晶体热力学和结构。 PXRD和SCXRD结果表明，它是在三斜晶系P -1 空间群中结晶的新共晶。热分析证实了 Phl-4B 共晶的纯度。 Phl-4B 共晶在 pH 1.2 中的平衡溶解度得到改善。体外模拟消化实验表明，Phl-4B 共晶的释放遵循 Fick 扩散。药物共结晶后根皮素的稳定性活性得到提高。 Phl-4B共晶的抗氧化性优于纯Phl。
更新日期：2024-07-08
中文翻译：
根皮素–4,4′-联吡啶共晶的药物特性：结构分析、药物释放曲线和抗氧化活性研究
为了提高根皮素的水溶性，我们采用溶剂蒸发法合成了Phl-4B共晶。采用各种分析技术，包括粉末 X 射线衍射 (PXRD)、热重分析 (TGA)、差示扫描量热法 (DSC)、傅里叶变换红外 (FTIR)、 1 HNMR 和单晶 X 射线衍射 (SCXRD)评估晶体热力学和结构。 PXRD和SCXRD结果表明，它是在三斜晶系P -1 空间群中结晶的新共晶。热分析证实了 Phl-4B 共晶的纯度。 Phl-4B 共晶在 pH 1.2 中的平衡溶解度得到改善。体外模拟消化实验表明，Phl-4B 共晶的释放遵循 Fick 扩散。药物共结晶后根皮素的稳定性活性得到提高。 Phl-4B共晶的抗氧化性优于纯Phl。
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