Method for extracting and separating paclitaxel and taxones compounds from yew

A technology of taxanes and paclitaxel, which is applied in the direction of organic chemistry and medical raw materials derived from gymnosperms, can solve the problems of difficult industrialization, high cost, and low yield, and solve the bottleneck problem of industrial production , The effect of improving the utilization rate

Inactive Publication Date: 2009-04-01
桂林市振达生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, only the extraction and semi-synthesis methods have achieved industrialization. Due to the complex structure of paclitaxel, the reported total synthesis methods have long routes, low yields, and high costs, and it is difficult to meet the requirements of industrialization.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 1) Get 10 kilograms of Taxus Mandia branches and leaves that are naturally dried in the shade, crush them to 40 mesh, extract them with 50 liters of ethanol with a volume concentration of 95% at room temperature for 5 hours, filter with 200 mesh filter cloth, and collect Extract; add 80 liters of ethanol with a volume concentration of 60% to extract for 10 hours, filter with a 200-purpose filter cloth, and collect the extract; add 50 liters of ethanol with a volume concentration of 55% for 8 hours, filter with a 200-purpose filter Cloth filter, collect extract; Merge extract, reclaim ethanol, extract is concentrated into 50 liters of extract;

[0019] 2) adding 50 liters of petroleum ether to the concentrated extract for deesterification three times, collecting the water layer, and concentrating to obtain the deesterified extract;

[0020] 3) The deesterified extract was extracted three times with 50 liters of ethyl acetate, and the organic phase and the aqueous phase o...

Embodiment 2

[0027] 1) Get 50 kilograms of southern yew branches and leaves that are naturally dried in the shade, crush them to 100 mesh, extract them at room temperature for 8 hours with 400 liters of ethanol with a volume concentration of 80%, filter with a filter cloth of 200 mesh, and collect the extract Add 250 liters of volume concentration again and be 75% ethanol extraction 10 hours, filter with 200 purpose filter cloth, collect extract; Add 300 liters of volume concentration again and be 20% ethanol extraction 10 hours, filter with 200 purpose filter cloth , collecting the extract; combining the extract, reclaiming ethanol, and concentrating the extract into 350 liters of extract;

[0028] 2) Add 350 liters of n-hexane deesterification three times to the concentrated extract, collect the water layer, and concentrate to obtain the deesterified extract;

[0029] 3) The deesterified extract was extracted three times with 350 liters of butyl acetate, and the organic phase and the aqu...

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PUM

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Abstract

The invention discloses a method for extracting and separating taxol and other taxane compounds from yew. The method includes the steps of extraction, degreasing, crude separation to an organic phase and an aqueous phase respectively, refined separation with reverse-phase chromatography, and crystallization. The invention sequentially adopts the ethanol of 80 to 95 percent, 60 to 75 percent and 20 to 55 percent to carry out gradient extraction to the yew material and also to fully extract taxane compounds with different polarities so as to lead the total extraction rate of the taxane compounds to be raised to more than 90 percent from 70 percent of the traditional art; the simultaneous extracting of 8 different tazane compound monomers from one set of the yew material is realized by the invention and the purity of each monomer can reach more than 98 percent; an aqueous phase substance which is generated in the extraction process abandoned by the traditional art is fully utilized to raise the utilization rate of the taxane compounds in the yew by 10 to 20 times, therefore, the bottleneck problem of industrial production of the lack of yew material is effectively solved.

Description

(1) Technical field: [0001] The invention relates to a method for extracting and separating paclitaxel and other taxane compounds from natural plants, in particular to a method for extracting and separating paclitaxel and other taxane compounds from yew. (two) background technology: [0002] Paclitaxel (trade name Taxol) is a diterpene compound isolated from Taxus genus with unique anticancer effect. It is widely used clinically in the chemotherapy of ovarian cancer, breast cancer, small cell and non-small cell lung cancer, esophageal cancer, head and neck cancer, chemotherapy-resistant leukemia and other cancers, and has definite curative effect. As the only new anticancer drug that promotes microtubule polymerization, taxol products Taxol and Taxotere have become one of the main anticancer drugs. The method for preparing paclitaxel includes: 1) extracting Taxol from yew or other renewable taxus plants; 2) semi-synthesizing Taxol or Taxotere from other natural taxane (10-d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14A61K36/13
Inventor 孙莉莉韦海洪梁晶唐江明李振志
Owner 桂林市振达生物制药有限公司
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