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紫杉醇初分离工艺中的除杂方法比较

The Comparison of Impurity Eliminations in Pretreatment of Paclitaxel Preparation

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【作者】 吴倩何克江杨义王正平杨凌

【Author】 WU Qian 2,HE Ke-jiang 1,YANG Yi 1,WANG Zheng-ping 2,YANG Ling 1*(1.Lab of Pharmaceutical Resource Discovery,Dalian Institute of Chemical Physics,Chinese Academy of Sciences,Dalian 116023,China;2.Chemistry Engineering Department,Harbin Engineering University,Harbin 150001,China)

【机构】 哈尔滨工程大学化工学院中国科学院大连化学物理研究所药用资源开发研究组中国科学院大连化学物理研究所药用资源开发研究组 哈尔滨150001大连116023哈尔滨150001大连116023

【摘要】 本文以除杂率、脱色率和紫杉醇回收率为定量指标,比较了萃取、碱液洗涤、酸碱液沉淀和离子交换树脂四种方法的优劣。对除杂率的评价,电导法结合TLC法较重量法更为客观。上述四种方法的电导法除杂率分别为73.4%、91.6%、30.7%和86.8%;脱色率分别为56.7%、75.9%、16.5%和71.8%,紫杉醇回收率分别为100%、159%、73.1%和152%。四种方法中,碱液洗涤法除杂效果最佳,紫杉醇回收率最高,此外,还具有操作简便、溶剂用量低、成本低和适合规模生产的优点。

【Abstract】 Four methods including liquid-liquid extraction,basic-solution extraction,acidic-basic precipitation and ion-exchange chromatography were applied in pretreatment of the paclitaxel purification and were compared in terms of impurity elimination rate,the decoloration rate and paclitaxel recovery.Impurity elimination was measured by three methods,Electrical Conductance (EC),Weighing and TLC,in which EC combined with TLC was evaluated as a better method.Impurity elimination rates by EC for four methods are 73.4%,91.6%,30.7% and 86.8%,the decoloration rates are 56.7%,75.9%,16.5% and 71.8%,and paclitaxel recoveries are 100%,159%,73.1% and 152%,respectively.In combination of TLC analysis,it is showed that basic-solution extraction is an optimal method and has achieved the highest paclitaxel recovery,which is 50% higher than that of chloroform liquid-liquid extraction method.As a result,this extraction method has the added advantage of requiring considerably less reagent and solvent,an attractive economical proposition for large scale production.

【基金】 国家重点基础研究发展计划(973计划)基金项目(2003CB716005)
  • 【文献出处】 天然产物研究与开发 ,Natural Product Research and Development , 编辑部邮箱 ,2005年03期
  • 【分类号】TQ461
  • 【被引频次】8
  • 【下载频次】413
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