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Increased stability and solubility of dihydroartemisinin in aqueous solution through the formation of complexes with 2-hydroxypropyl-β-cyclodextrin 被引量:3

2-羟丙基-β-环糊精(HP-β-CD)对双氢青蒿素水溶液的稳定性和溶解性的影响(英文)
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摘要 The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) on the solubility of dihydroartemisinin (DHA) in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β- eyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ℃ was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin. 各种不同浓度的2-羟丙基-β-环糊精对双氢青蒿素的不同pH值水溶液的溶解度的影响进行了研究。不同浓度的2-羟丙基-β-环糊精对双氢青蒿素在50,60,70,80oC条件下的稳定性也进行了研究。制备了双氢青蒿素2-羟丙基-β-环糊精包合物并通过X-射线衍射和差示热分析验证了包合物已经形成。2-羟丙基-β-环糊精有效地抑制了双氢青蒿素的水解,而且,2-羟丙基-β-环糊精的浓度越高,双氢青蒿素的溶解度和稳定性越好温度越高,双氢青蒿素的稳定性越差。2-羟丙基-β-环糊精是双氢青蒿素的增稳剂和增溶剂。
出处 《Journal of Chinese Pharmaceutical Sciences》 CAS 2009年第2期170-176,共7页 中国药学(英文版)
关键词 DIHYDROARTEMISININ 2-HYDROXYPROPYL-Β-CYCLODEXTRIN SOLUBILITY STABILITY 双氢青蒿素 2-羟丙基-β-环糊精 溶解性 稳定性
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  • 1Kazufumi Shiotani,Keiko Uehata,Tetsumi Irie,Kaneto Uekama,Diane O. Thompson,Valentino J. Stella. Differential Effects of Sulfate and Sulfobutyl Ether of β-Cyclodextrin on Erythrocyte Membranes in Vitro[J] 1995,Pharmaceutical Research(1):78~84
  • 2Abdi Y. Tinwalla,Barbara L. Hoesterey,Tian-xiang Xiang,Kap Lim,Bradley D. Anderson. Solubilization of Thiazolobenzimidazole Using a Combination of pH Adjustment and Complexation with 2-Hydroxypropyl-β-Cyclodextrin[J] 1993,Pharmaceutical Research(8):1136~1143
  • 3Fang-yu Liu,Dane O. Kildsig,Ashim K. Mitra. Cyclodextrin/Weak-Electrolyte Complexation: Interpretation and Estimation of Association Constants from Phase Solubility Diagrams[J] 1992,Pharmaceutical Research(12):1671~1672
  • 4Bernd W. Müller,Ulrich Brauns. Change of Phase-Solubility Behavior by Gamma-Cyclodextrin Derivatization[J] 1985,Pharmaceutical Research(6):309~310

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