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落新妇苷-β-环糊精包结物的溶解性及生物利用度研究 被引量:2

Solubility and in vivo Bioavailability of Astilbin-β-cyclodextrin Complexes
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摘要 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%。 The inclusion reaction of astilbin with β-cyclodextrin(β-CD) was investigated by UV spectrometry in this study.β-CD could form complex with astilbin in ratio of 1:1 with formation constant of 1788.54±273.41 M-1,and gradually decrease the absorbance of astilbin at 291 nm.The complex was prepared by co-grinding method.The effects of water content and molar ratio on inclusion rate during grind were investigated.The results showed that properly increasing of water content and β-CD molar ratio enhanced the formation of astilbin complexes.Finally,the solubility and in vivo bioavailability of astilbin and its β-CD complexes prepared with molar ratio of 1:2 were investigated.The solubility of astilbin in β-CD complexes was increased 106.14 times and its dissolution profiles were improved.The in vivo bioavailability study showed that β-CD enhanced the absorb rate of astilbin,shortened Tmax and increased Cmax.However,the absolute bioavailability between astilbin and its β-CD complexes had no difference,and were both around 3.7%.
出处 《现代食品科技》 EI CAS 北大核心 2014年第5期82-86,共5页 Modern Food Science and Technology
基金 江西省自然科学基金资助项目(20122BAB214005) 江西农业大学青年基金资助项目(QN201108)
关键词 落新妇苷 Β-环糊精 包结物 溶解度 生物利用度 astilbin β-cyclodextrin complexes solubility bioavailability
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参考文献13

  • 1张清峰,聂海纯,郑国栋,上官新晨.落新妇苷的理化性质与生物活性研究进展[J].现代食品科技,2012,28(12):1834-1838. 被引量:14
  • 2Landrault N, Larronde F, Delaunay J C, et al. Levels of stilbene oligomers and astilbin in french varietal wines and in grapes during noble rot development [J]. Journal of Agricultural and Food Chemistry, 2002, 50: 2046-2052.
  • 3Fei M J, Wu X F, Xu Q. Astilbin inhibits contact hypersensitivity through negativecytokine regulation distinct from cyclosporin [J]. Journal of Allergy and Clinical Immunology, 2005, 116: 1350-1356.
  • 4Guo J M, Qian F, Li J X, et al. Identification of a new metabolite of astilbin, 3\'-O-methylastilbin, and its immunosuppressive activity against contact dermatitis [J]. Clinical chemistry, 2007, 53: 465-471.
  • 5Cai Y, Chen T, Xu Q. Astilbin suppresses collagen-induced arthritis via the dysfunction of lymphocytes [J]. Inflammation Research, 2003, 52: 334-340.
  • 6Xu Q, Wu F G, Cao J S, et al. Astilbin selectively induces dysfunction of liver-infiltrating cells-novel protection from liver damage [J]. European Journal of Pharmacology, 1999, 377: 93-100.
  • 7徐强,孙洋.源于中药选择性效应的新型免疫抑制疗法[J].化学进展,2009,21(1):55-62. 被引量:19
  • 8Zhang Q F. The Quantitative study, fingerprint analysis and biological effect of rhizoma smilacis glabrae [D]. Doctoral thesis, City University of Hong Kong, 2010.
  • 9Martin Del Valle E M. Cyclodextrins and their uses: a review [J]. Process Biochemistry, 2004, 39: 1033-1046.
  • 10Yuichi T, Arpansiree W, Keiko S, et al. Co-grinding with cyclodextrin as a nanoparticle preparation method of a poorly water soluble drug [J]. Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2004, 50: 67-71.

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