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葛根素/β-环糊精包合物的初步研究

An preliminary study of inclusion complex of puerarin andβ-cyclodextrin

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【作者】 董祥玉任勇马学琴王敏

【Author】 DONG Xiang-yu,REN Yong.MA Xue-qin,WANG Min ( Center of Drug Discovery, Nanjing Normal University, Nanjing 210097 , China)

【机构】 南京师范大学新药研究中心南京师范大学新药研究中心 南京210097南京210097

【摘要】 目的:制备葛根素/β-环糊精包合物,并考察其溶解度。方法:用捏合法制备葛根素/β-环糊精包合物,采用紫外光谱法和相溶解度法研究包合过程,差示扫描量热分析、X-衍射、1H-NMR验证包合物,并测定了包合物的溶解度。结果:葛根素与β-环糊精可形成1:1(物质的量比)的稳定包合物,包合常数398 L·mol-1。37℃下包合物使葛根素的溶解度增加5.55倍。结论:β-环糊精对葛根素增溶作用明显,适用于葛根素口服制剂的改进。

【Abstract】 Objective:To investigate the preparation and solubility of the inclusion complex of puerarin andβ-cyclodextrin. Methods: The inclusion complex of puerarin andβ-cyclodextrin was prepared using a kneading technique. The inclusion process was monitored by ultraviolet spectroscopy and phase solubility-test. The inclusion complex was validated by DTA, XRD and1 H-NMR. The solubility of the complex was measured using phase solubility analysis. Results: Puerarin formed an optimal inclusion complex withβ-cyclodextrin at a molar ratio of 1: 1, which had an equilibrium constant of 398 L·mol-1. The solubility of puerarin was increased by 5.55 times in presence of one molar ofβ-cyclodextrin at 37℃. Conclusion :β-cyclodextrin seemed an ideal soluble enhancer of oral puerarin preparations.

  • 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2006年07期
  • 【分类号】R283
  • 【被引频次】23
  • 【下载频次】486
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