共晶改善黄酮类化合物成药性能的研究进展
Research progress in cocrystal improvement of druggable properties of flavonoids
尹苗苗 1尚海花 2侯越 2陶铭 3李祎亮 2侯文彬2
作者信息
- 1. 天津中医药大学,天津 301617
- 2. 北京协和医学院&中国医学科学院放射医学研究所,天津市放射医学与分子核医学重点实验室,天津 300192
- 3. 沈阳药科大学,辽宁 本溪 117004
- 折叠
摘要
黄酮类化合物是一类天然有机化合物,种类和数量众多,因具有广泛的药理活性而备受关注,已经成为国内外天然药物开发和研究的热点.然而,黄酮类化合物本身存在着水溶性差、生物利用度低和在体内不稳定等问题,限制了其临床应用.由于黄酮类化合物中通常缺乏可电离的基团,共晶策略是提高这些化合物的溶解度和生物利用度的有效方法.笔者对近年来成功制备的黄酮类化合物共晶对其原料药物溶解度、溶出速率、渗透性、生物利用度等方面的影响进行综述,并简要介绍其改变机制,以期为黄酮类化合物共晶产品的进一步开发与深入研究提供参考.
Abstract
Flavonoids are natural organic compounds with many types and quantities.They have attracted much attention due to their extensive pharmacological activities,and have become a hot spot in the development and research of natural drugs at home and abroad.However,flavonoids also have problems such as poor water solubility,low bioavailability and instability in vivo,which limit their clinical application.Because flavonoids usually lack ionizable groups,cocrystal strategy is often an effective way to improve the solubility and bioavailability of these compounds.The effects of flavonoids cocrystal successfully prepared in recent years on the solubility,dissolution rate,permeability and bioavailability of raw materials were reviewed and its mechanism was briefly introduced to provide reference for further development and in-depth research of flavonoids cocrystal products.
关键词
黃酮类化合物/共晶/成药性能/改变机制Key words
flavonoid/cocrystal/druggable property/mechanism of change引用本文复制引用
基金项目
国家自然科学基金(82104012)
国家自然科学基金(82202950)
中国医科院医学与健康科技创新工程国家医学健康科技战略平台与体系建设专项(2022-I2M-2-003)
天津市自然科学基金(22JCQNJC00690)
中央高校基本科研业务费专项(3332022063)
出版年
2024