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本文通过紫外吸收光谱法研究了落新妇苷与β-环糊精(β-CD)的包结反应。β-CD可与落新妇苷形成1:1包结物,并使其在291 nm处吸光度有规律下降,二者包结平衡常数为1788.54±273.41 M-1。采用研磨法制备落新妇苷与β-CD的包结物,考察了水分含量和摩尔比对落新妇苷包结率的影响。适当提高研磨过程中水份含量和β-CD摩尔比可增加落新妇苷包结率。最后,比较了β-CD包结物和落新妇苷单体的溶解度、体外溶出度和大鼠体内生物利用度。形成β-CD包结物可显著提高落新妇苷溶解度。25℃条件下,包结物中落新妇苷的溶解度为52.01 mM,为落新妇苷单独存在时的106.14倍。体外溶出度曲线表明包结物中落新妇苷的溶解速度更快。包结物中落新妇苷在大鼠体内达到峰值时间更短,且峰值浓度更高,但二者生物利用度相当,绝对生物利用度都约为3.7%。
In this paper, the inclusion reaction of astilbin and β-cyclodextrin (β-CD) was studied by ultraviolet absorption spectroscopy. β-CD forms a 1: 1 inclusion complex with astilbin, and its absorbance decreases regularly at 291 nm. The entrapment equilibrium constant of β-CD is 1788.54 ± 273.41 M-1. The inclusion complex of astilbin and β-CD was prepared by grinding method. The effects of water content and molar ratio on the entrapment efficiency of astilbin were investigated. Appropriate to improve the water content in the grinding process and β-CD molar ratio can increase neosidine incorporation rate. Finally, the solubility, in vitro dissolution and in vivo bioavailability of β-CD inclusion and astilbin monomers were compared. Formation of β-CD inclusion significantly improves the solubility of astilbin. The solubility of astilbin in inclusion complex was 52.01 mM at 25 ℃, which was 106.14 times higher than that of astilbin alone. The in vitro dissolution profile shows that astilbin in the inclusion complex dissolves more rapidly. Inclusion of astilbin in rats peaked shorter time and higher peak concentrations, but the two bioavailability quite, the absolute bioavailability of about 3.7%.