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固体分散体中葛根素与磷脂的相互作用

翟光喜*, 娄红祥, 毕殿洲, 邹立家   

  1. 1.山东大学药学院, 济南 250012;
    2.沈阳药科大学药学院, 沈阳 110015
  • 收稿日期:2002-06-06 修回日期:2003-02-10 出版日期:2003-03-15 发布日期:2003-03-15
  • 通讯作者: 翟光喜*

Interaction of Puerarin with Phospholipid in Solid Dispersion

ZHAI Guang-xi*, LOU Hong-xiang, BI Dian-zhou, ZOU Li-jia   

  1. 1.School of Pharmacy, Shandong University, Jinan 250012, China;
    2.School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110015, China
  • Received:2002-06-06 Revised:2003-02-10 Online:2003-03-15 Published:2003-03-15
  • Contact: ZHAI Guang-xi*

摘要: 目的 研究葛根素与磷脂在固体分散体中的作用.方法 溶剂挥发法制备固体分散体, 通过紫外、红外、核磁共振光谱和薄层层析研究了葛根素与磷脂在固体分散体中的作用.结果 在氯仿中葛根素及其物理混合物的最大紫外吸收波长为243 nm, 但固体分散体为250 nm, 而在甲醇中都为250 nm.与物理混合物相比, 固体分散体中葛根素苯环骨架的特征吸收峰和磷脂P=O伸缩振动峰明显改变, 磷脂的C=C伸缩振动峰消失; 在核磁共振光谱中固体分散体中葛根素苯环骨架的信号明显减弱或消失, 而磷脂极性端和不饱和部分的信号明显变化.在以氯仿甲醇水(65:25:5)为展开剂的硅胶薄层板上葛根素与磷脂可完全分开.结论 在固体分散体中葛根素的苯环骨架与磷脂极性端和不饱和部分可能以氢键、静电引力或电荷迁移力以及分子间作用力相作用而固定, 并被磷脂的脂肪链所包围.

关键词: 葛根素, 磷脂, 固体分散体, 核磁共振

Abstract: Aim To study the interaction of puerarin (PU) with phospholipid (PL) in solid dispersion. Methods PU/PL solid dispersion was prepared with solvent evaporation and the interaction between PU and PL was studied by analysis of their ultraviolet spectra, infrared spectra, 1H NMR spectra and thin layer chromatogram. Results In chloroform the maximum absorption peak of PU in PU/PL mixture was located at 243 nm, but 251 nm for that of PU in solid dispersion. However in methanol, QU in mixture or solid dispersion had the same maximum absorption peak location in ultraviolet spectra. Compared with the infrared spectra of mixture, that of solid dispersion showed the specific absorption peak location of benzene ring framework in PU molecule was markedly changed, the stretching vibration peak of P=O in PL molecule was shifted to high wave numbers and the stretching vibration peak of C=C in PL molecule was disappeared. In 1H NMR spectra, most of the signals from PU in solid dispersion were weaken markedly or disappeared and the signals from the polar partof PL molecule were significantly changed. PU and PL in solid dispersion could be separated on silica gel plate with the mixed solvent of chloroform, methanol and water (65:25:5) or ethyl acetate and methanol (10:1). Conclusion In soliddispersion the benzene ring framework of PU molecule could act with the polar part and unsaturated part of PL moleculethrough charges fransfer, and the interacted part could be surrounded by fat chains of PL molecule.

Key words: puerarin, puerarin, phospholipid, phospholipid, solid dispersion, solid dispersion, nucleus magnetic resonance, nucleus magnetic resonance

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Supporting: *Corresponding author. 86-0531-8382015