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

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

张晓云, 刘建平^*, 乔华, 黄奎源, 史彦斌, 宋淑梅, 倪京满

1. 中国药科大学药学院, 江苏南京 210009
2. 兰州大学药学院, 甘肃兰州 730000
3. 兰州大学第一医院药剂科, 甘肃兰州 730000

收稿日期:2009-03-25 修回日期:2009-05-10 出版日期:2009-06-15 发布日期:2009-06-15
通讯作者: 刘建平*

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

Xiao-Yun Zhang, Jian-Ping Liu*, Hua Qiao, Kui-Yuan Huang, Yan-Bin Shi, Shu-Mei Song, Jing-Man Ni

1. College of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
2. College of Pharmacy, Lanzhou University, Gansu 730000, China
3. Department of Pharmaceutics, the First Hospital of Lanzhou University, Gansu 730000, China

Received:2009-03-25 Revised:2009-05-10 Online:2009-06-15 Published:2009-06-15
Contact: Jian-Ping Liu*

摘要/Abstract

摘要：

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, 80 ºC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。

关键词: 双氢青蒿素, 2-羟丙基-β-环糊精, 溶解性, 稳定性

Abstract:

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-cyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ºC 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.

Key words: Dihydroartemisinin, Dihydroartemisinin, 2-Hydroxypropyl-β-cyclodextrin, 2-Hydroxypropyl-β-cyclodextrin, Solubility, Solubility, Stability, Stability

中图分类号:

R917

Supporting:

^*Corresponding author. Tel./fax: 86-25-85339924;

e-mail: Liujianpingljp@hotmail.com

张晓云, 刘建平^*, 乔华, 黄奎源, 史彦斌, 宋淑梅, 倪京满. 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[J]. .

Xiao-Yun Zhang, Jian-Ping Liu*, Hua Qiao, Kui-Yuan Huang, Yan-Bin Shi, Shu-Mei Song, Jing-Man Ni. Increased stability and solubility of dihydroartemisinin in aqueous solution through the formation of complexes with 2-hydroxypropyl-β-cyclodextrin [J]. .

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