槲皮素-磷脂-鱼精蛋白复合物的制备及其体外释放度评价

丁淑敏, 隋鸣, 杨莹, 毛明强, 封亮, 宋国强

中国药学杂志 ›› 2022, Vol. 57 ›› Issue (23) : 2024-2029.

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中国药学杂志
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中国药学杂志 ›› 2022, Vol. 57 ›› Issue (23) : 2024-2029. DOI: 10.11669/cpj.2022.23.010
论著

槲皮素-磷脂-鱼精蛋白复合物的制备及其体外释放度评价

  • 丁淑敏1, 隋鸣1, 杨莹1, 毛明强1, 封亮2, 宋国强1*
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Preparation and Evaluation on the in Vitro Release of Quercetin-Phospholipid-Protamine Compound

  • DING Shu-min1, SUI Ming1, YANG Ying1, MAO Ming-qiang1, FENG Liang2, SONG Guo-qiang1*
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摘要

目的 以大豆卵磷脂和鱼精蛋白为辅料制备复合物,提高槲皮素的溶解性及体外释放度。方法 设计正交实验筛选制备槲皮素-磷脂复合物的最优制备条件;参照正交实验的工艺制备槲皮素-磷脂-鱼精蛋白复合物,并采用热重分析(TG)、X-射线衍射分析(XRD)、红外光谱分析(IR)对其进行表征;以HPLC对槲皮素及其复合物进行体外溶出度测定。结果 制备槲皮素-磷脂复合物的最优条件为投料比1∶2,质量浓度3 mg·mL-1,时间2 h,温度50 ℃;槲皮素-磷脂-鱼精蛋白复合物表征发现槲皮素由晶型变为无定型状态存在于复合物中;复合物呈均一粉末状固体;体外释放度结果表明槲皮素-磷脂-鱼精蛋白复合物中槲皮素的释放度显著提高,180 min累积释放度由29.96%提高到91.50%。结论 以大豆卵磷脂、鱼精蛋白为辅料制备的槲皮素-磷脂-鱼精蛋白复合物改变了槲皮素的存在状态,有效提高了槲皮素的体外释放度。

Abstract

OBJECTIVE To prepare the quercetin-phospholipid-protamine compounds with soy lecithin and protamine as auxiliary materials, then improve the solubility and in vitro release characteristics of quercetin. METHODS The quercetin-phospholipid-protamine compounds were prepared under the optimized experimental conditions obtained by orthogonal experiments. The compounds were characterized by TG, XRD and IR. The test on the in vitro release of quercetin and its compounds were performed by HPLC. RESULTS The conditions for preparing the quercetin-phospholipid compounds were optimized with the feed ratio and the concentration being 1∶2 and 3 mg·mL-1 respectively, under the temperature of 50 ℃ for 2 hrs. It was found that the quercetin existed in an amorphous state in the compounds. The prepared powders possess homogeneous microstructures. The in vitro release test found that the dissolution of quercetin in quercetin-phospholipid-protamine compounds were significantly improved from 29.96% to 91.50% within 180 min. CONCLUSION Soy lecithin and protamine as auxiliary materials changed the phase state of quercetin from crystal to amorphous, which effectively improves the solubility and in vitro release of quercetin.

关键词

槲皮素 / 大豆卵磷脂 / 鱼精蛋白 / 复合物 / 体外释放度

Key words

quercetin / phospholipid / protamine / compound / in vitro release

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丁淑敏, 隋鸣, 杨莹, 毛明强, 封亮, 宋国强. 槲皮素-磷脂-鱼精蛋白复合物的制备及其体外释放度评价[J]. 中国药学杂志, 2022, 57(23): 2024-2029 https://doi.org/10.11669/cpj.2022.23.010
DING Shu-min, SUI Ming, YANG Ying, MAO Ming-qiang, FENG Liang, SONG Guo-qiang. Preparation and Evaluation on the in Vitro Release of Quercetin-Phospholipid-Protamine Compound[J]. Chinese Pharmaceutical Journal, 2022, 57(23): 2024-2029 https://doi.org/10.11669/cpj.2022.23.010
中图分类号： R944   

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基金

国家自然科学基金项目资助(81603336)
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