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

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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

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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