β-双氢青蒿素在不同溶剂中的核磁共振研究

目的研究β-双氢青蒿素在不同测试溶剂中的转化并对其核磁共振信号进行全归属。方法利用HSQC,HMBC等二维核磁共振技术,对β-双氢青蒿素进行测试,利用1H-NMR研究双氢青蒿素β-体与α-体的相互转化。结果首次利用二维核磁共振技术对β-双氢青蒿素的核磁共振信号进行了全归属,β-双氢青蒿素在DMSO中只以β-体一种构型存在。结论β-双氢青蒿素在DMSO中不存在异构体的转化,其核磁信号可以以DMSO-d6为溶剂而得到准确归属。

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

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.