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制备山奈酚磷脂复合物以提高其溶解度和抗高尿酸血症活性。

Preparation of an isorhamnetin phospholipid complex for improving solubility and anti-hyperuricemia activity.

机构信息

School of Traditional Chinese Material Medica, Shenyang Pharmaceutical University, Shenyang, China.

Faculty of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang, China.

出版信息

Pharm Dev Technol. 2022 Sep;27(7):842-852. doi: 10.1080/10837450.2022.2123510. Epub 2022 Sep 16.

Abstract

To improve the solubility and anti-hyperuricemia activity of the insoluble natural flavonoid isorhamnetin (ISO), an isorhamnetin phospholipid complex (ISO-PC) was prepared. ISO-PC was prepared through solvent evaporation and its prescription process was optimized. The formation of ISO-PC was verified via multiple characterization methods. Parameters such as drug loading, solubility, octanol-water partition coefficient, stability, and anti-hyperuricemia activity of ISO-PC were investigated. The complexation efficiency of ISO-PC was 95.1% ± 0.56%. The characterization results confirmed that ISO-PC was bound by intermolecular interactions between ISO and phospholipids. Compared with ISO, the solubility of ISO-PC in water and 1-octanol increased by 122 and 16.5 times, respectively. In addition, the octanol-water partition coefficient decreased to 1.08. Pharmacodynamic studies have reported that ISO-PC has a more significant effect on reducing serum uric acid levels and renal protection. In conclusion, the findings of this study suggested that ISO-PC could be used as a promising formulation to improve the solubility and the anti-hyperuricemia activity of ISO.

摘要

为提高不溶性天然类黄酮山柰素(ISO)的溶解度和抗高尿酸血症活性,制备了山柰素磷脂复合物(ISO-PC)。通过溶剂蒸发法制备 ISO-PC,并对其处方工艺进行优化。采用多种表征方法验证了 ISO-PC 的形成。考察了 ISO-PC 的载药量、溶解度、油水分配系数、稳定性和抗高尿酸血症活性等参数。ISO-PC 的包合效率为 95.1%±0.56%。表征结果证实 ISO-PC 是通过 ISO 和磷脂分子间的相互作用结合而成。与 ISO 相比,ISO-PC 在水中和 1-辛醇中的溶解度分别提高了 122 倍和 16.5 倍。此外,油水分配系数降低至 1.08。药效学研究报道,ISO-PC 对降低血尿酸水平和肾脏保护作用更显著。综上所述,本研究结果表明,ISO-PC 可作为提高 ISO 溶解度和抗高尿酸血症活性的一种有前途的制剂。

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