Xue Fumin, Yuan Xinyue, Li Xingyi, Fang Shimin, Cheng Yan
Shandong Analysis and Test Center, School of Pharmaceutical Sciences, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250014, China.
School of Material Science and Engineering, Shandong Jianzhu University, Jinan 250101, China.
Int J Mol Sci. 2025 Apr 30;26(9):4266. doi: 10.3390/ijms26094266.
Improving the stability of drugs in the solid state, as well as improving their solubility and poor bioavailability, is highly physiologically relevant. In this study, we focused on enhancing the solubility of hypoxanthine (HYP) through salt formation resulting from the preparation of hypoxanthine-maleic acid salt (HYP-MAL). Single crystals were obtained through solvent evaporation methods, and DSC, TGA, PXRD, FT-IR, and H NMR spectra were used to characterize the samples. The salt system had higher solubility properties than HYP, with an equilibrium solubility in water that was roughly 2.4 times greater than that of HYP, but the salt's equilibrium solubility increased when the pH shifted from 7.4 to 1.2; additionally, from 0 to 10 min, the powder dissolution rate was 1.8 times that of HYP, resulting in increased bioavailability. The anti-obesity impact of HYP-MAL salt on obese mice was investigated, providing important insights for the development of future weight-loss medications.
提高药物在固态下的稳定性，以及改善其溶解性和低生物利用度，具有高度的生理相关性。在本研究中，我们专注于通过制备次黄嘌呤-马来酸盐（HYP-MAL）形成盐来提高次黄嘌呤（HYP）的溶解度。通过溶剂蒸发法获得单晶，并使用DSC、TGA、PXRD、FT-IR和H NMR光谱对样品进行表征。该盐体系比HYP具有更高的溶解性，在水中的平衡溶解度约为HYP的2.4倍，但当pH从7.4变为1.2时，该盐的平衡溶解度增加；此外，在0至10分钟内，粉末溶解速率是HYP的1.8倍，从而提高了生物利用度。研究了HYP-MAL盐对肥胖小鼠的抗肥胖作用，为未来减肥药物的开发提供了重要见解。
