食品科学 ›› 2013, Vol. 34 ›› Issue (8): 89-93.doi: 10.7506/spkx1002-6630-201308018

• 工艺技术 • 上一篇    下一篇

环糊精对青蒿素的包合工艺研究

段友构,朱士龙,张浚生,李勇   

  1. 吉首大学化学化工学院,湖南 吉首 416000
  • 收稿日期:2011-12-09 修回日期:2013-02-20 出版日期:2013-04-25 发布日期:2013-05-07
  • 通讯作者: 朱士龙 E-mail:elicss@163.com
  • 基金资助:
    湖南省自然科学基金资助项目;湖南省教育厅资助项目;民族药用植物资源研究与利用湖南省重点实验室开放基金项目;吉首大学校级科研项目

Optimization of Inclusion Reactions of β-Cyclodextrin and Its Derivatives with Artemisinin

DUAN You-gou,ZHU Shi-long,ZHANG Jun-sheng,LI Yong   

  1. College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China
  • Received:2011-12-09 Revised:2013-02-20 Online:2013-04-25 Published:2013-05-07
  • Contact: elicss E-mail:elicss@163.com

摘要: 通过单因素及正交试验确定青蒿素与3种环糊精形成包合物的最佳条件,在此条件下利用相溶解度法测定青蒿素与β-环糊精、羟丙基-β-环糊精、γ-环糊精的包合常数并计算包合反应前后的吉布斯自由能。结果表明:青蒿素与环糊精形成包合物的最佳条件为配比1:1(mol/mol)、包合温度40℃、包合时间5h、包合反应时溶液pH7,青蒿素与β-环糊精、羟丙基-β-环糊精、γ-环糊精的包合常数分别为80.06、58.68、116.96L/mol,反应前后的吉布斯自由能变化分别为-11.76、-10.93、-12.78kJ/mol。表明青蒿素与环糊精可以形成1:1型稳定的包合物,环糊精可以增大青蒿素的溶解度。

关键词: 青蒿素, 环糊精, 包合常数, 正交试验设计, 工艺优化

Abstract: One-factor-at-a-time method and orthogonal array design were used to establish the optimal reaction conditions for inclusion complexes of β-cyclodextrin and its derivatives with artemisinin. Formation constants for inclusion complexes of artemisinin with β-cylcodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD) and γ-cyclodextrin (γ-CD) were measured by phase solubility analysis and Gibbs free energy differences were also calculated before and after reactions. The optimal reaction conditions for artemisinin/cyclodextrin inclusion complexes were 1:1, 40 ℃, 5 h and 7 for artemisinin-to-cyclodextrin molar ratio, temperature, reaction time and medium pH, respectively. The formation constants of the inclusion complexes of artemisinin with β-CD, HP-β-CD and γ-CD were 80.06, 58.68 L/mol and 116.96 L/mol, respectively, and the corresponding Gibbs free energy differences were -11.76, -10.93 kJ/mol and -12.78 kJ/mol, respectively. In this study, we have succeeded in preparing 1:1 artemisinin/cyclodextrin inclusion complexes with improved solubility of artemisinin.

Key words: artemisinin, cyclodextrin, inclusion constant, orthogonal array design, process optimization

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