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首页> 外文期刊>RSC Advances >Preparation of quercetin–nicotinamide cocrystals and their evaluation under in vivo and in vitro conditions
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Preparation of quercetin–nicotinamide cocrystals and their evaluation under in vivo and in vitro conditions

机译：在体内和体外条件下制备槲皮素 - 烟酰胺酰胺酰胺酰胺和它们的评价

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Quercetin is a flavonoid abundant in the plant kingdom. Various types of bioactivities of quercetin have been demonstrated in vitro . Although quercetin has been proposed to exhibit numerous pharmacological benefits, it suffers from low bioavailability on account of its obviously poor solubility in water. Cocrystals have generated interest recently as a way of enhancing the dissolution in vitro and creating relative bioavailability of insoluble medicine. In this study, quercetin–nicotinamide cocrystals were obtained via a solvent evaporation technique. Furthermore, quercetin–nicotinamide cocrystals were characterized via Fourier transform infrared (FI-IR) spectroscopy, X-ray powder diffraction (PXRD), and differential scanning calorimetry (DSC) techniques. Quercetin–nicotinamide cocrystals are a new phase material, and the established intermolecular forces such as hydrogen bonds between quercetin and nicotinamide existed in the quercetin–nicotinamide cocrystals, as confirmed from the solid-state analysis. The dissolution of quercetin–nicotinamide cocrystals was found to be significantly higher than that of quercetin crystals. The pharmacokinetic data from the in vivo experiments suggested that quercetin–nicotinamide cocrystals could significantly increase the oral absorption of quercetin by nearly 4-fold. These results demonstrate that the developed quercetin–nicotinamide cocrystals are a promising oral formulation toward improvement in the dissolution and bioavailability of quercetin.
机译：槲皮素是植物王国中的黄酮类化合物。已经在体外证明了槲皮素的各种类型的生物活性。虽然已经提出了槲皮素表现出许多药理益处，但由于其在水中明显贫瘠的溶解度，它具有低生物利用度。距离克里克里斯人最近产生了利益作为增强体外溶解的一种方式，并产生不溶性药物的相对生物利用度。在该研究中，通过溶剂蒸发技术获得槲皮素 - 烟酰胺酰胺酰胺。此外，通过傅里叶变换红外（FI-IR）光谱，X射线粉末衍射（PXRD）和差示扫描量热法（DSC）技术表征了槲皮素 - 烟酰胺酰胺。槲皮素 - 烟酰胺酰胺酰基烯库是一种新的相材料，并且在槲皮素 - 烟酰胺酰胺酰胺中存在槲皮素和烟酰胺之间的氢键如氢键，如从固态分析所证实的那样。发现槲皮素 - 烟酰胺酰胺酰胺的溶解明显高于槲皮素晶体的溶解。来自体内实验的药代动力学数据表明，槲皮素 - 烟酰胺酰胺酰基晶体可以显着增加槲皮素的口服吸收近4倍。这些结果表明，发育的槲皮素 - 烟酰胺酰胺酰基烯库是有望的口服配方，旨在改善槲皮素的溶解和生物利用度。

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