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反相高效液相色谱分离青蒿素及其衍生物

SEPARATION OF ARTEMISININE AND ITS DERIVATIVES BY REVERSED PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

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【作者】 张仁斌徐松林李英

【Author】 Zhang Renbin (J P Chang), Xu Songlin and Li Ying (Shanghai Institute of materia Medica, Academia Sinica)

【机构】 中国科学院上海药物研究所中国科学院上海药物研究所

【摘要】 本文应用反相高效液相色谱研究了抗疟新药青蒿素、还原青蒿素及其醚、羧酸酯、碳酸酯等各种衍生物的分离条件和色谱性质。这些化合物及其差向异构体在十八烷基键合固定相(GYT-C18)上用甲醇—水作定比冲洗(Isocratic elution)可得到完全分离,并可用内径10mm填充同样填料的层析柱进行小量制备分离。 在研究上述化合物的色谱保留值与疏水性的关系时发现,容量因素k′随取代基疏水性的增加而增加,logk′与代表取代基疏水性的疏水取代基参数π之间存在着线性相关性。此外,logk′与烷基取代基的链长之间也有线性关系。 冲洗液中的甲醇浓度与logk′之间也存在着相反的线性关系。

【Abstract】 The chromatographic behaviors of new antimalarial drugs artemisinine, dihydroartemisinine and its ethers, carboxylic esters, carbonates have been studied using reversed phase high performance liquid chromatography. These compounds and their epimers can be completely separated on the octadecylsilane bonded stationary phase GYT-C18 under isocratic condition with methanol-water as eluant and semipreparative separation may also be carried out by a I. D. 10 mm column packed with the same packing material.In studying the relationship between the retention and hydrophobicity of the above mentioned compounds, it was observed that, the capacity ratio k’ increases with increase of the substituent’s hydrophobicity, and the correlation of the logarithm of capacity ratio k’ with Hansch’s hydrophobic substituent parameter was established. Futhermore, the linearity between log k’ and chain-length of the alkyl substituent was also obtained.The effect of the solvent composition on the retention time has been studied. The value of log k’ decreases linearly with increase of the concentration of methanol in eluent.

  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1981年06期
  • 【被引频次】13
  • 【下载频次】199
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