落新妇苷的稳定性、药动学及制剂学研究进展

Research Progress on Stability,Pharmacokinetics and Dosage Forms of Astilbin

落新妇苷是来源于土茯苓、黄杞等中药的一种二氢黄酮类化合物,具有选择性免疫抑制、抗炎、抗氧化、降血糖、神经保护、预防骨丢失等多种药理活性,然而其稳定性差、水溶性低、生物利用度极低,限制临床应用。综述近年来落新妇苷稳定性、药物动力学和制剂学等相关研究进展,归纳出导致落新妇苷稳定差和生物利用度低的主要原因为异构化与分解、溶解性差、半衰期短、P-糖蛋白(P-gp)外排作用等,总结中药配伍对落新妇苷生物利用度的影响,为进一步深入开发利用落新妇苷提供参考。

Astilbin is a naturally occurring dihydroflavonol,presented in Tufuling(Rhizoma Smilacis Glabrae),Huangqi(En⁃gelhardia roxburghiana),etc.Astilbin was reported to possess unique selective immunosuppressive activity,anti-inflammation,antioxidant,hypoglycemic effect,neuroprotection,prevention of bone loss and so on.However,poor stability,low water-soluble and oral bioavailability of astilbin has restricted its development.This review made a comprehensive summary of the study on sta⁃bility,pharmacokinetics and pharmaceutics research of astilbin in recent decades,and concluded that the main reasons for poor stability and low bioavailability were easy isomerization and degradation,poor solubility,short half-life and P-gp efflux effect.Furthermore,the compatibility effect of traditional Chinese medicine on the bioavailability of astilbin was summarized.This review aimed to facilitate further research and development of astilbin.