Method for extracting paclitaxel from taxus chinensis branch and leaf

A technology of yew branches and leaves, paclitaxel, applied in the direction of organic chemistry, can solve the problems of low extraction efficiency, unsatisfactory purification effect, unsuitable paclitaxel, etc., and achieve the effect of reducing extraction cost, complete separation and easy operation

Active Publication Date: 2013-06-26
SICHUAN XIANGGUANG AGRI TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the yew branches and leaves contain a large amount of impurities such as pigments, waxy oils and similar substances, these impurities make the separation and extraction of paclitaxel more complicated, and the traditional method of extracting paclitaxel from the bark of yew is not applicable at all.
For this reason, major enterprises in this field have spent huge sums of money to organize scientific researchers to carry out a large number of repeated studies, and various research results have been frequently reported in public publications, such as "a kind of yew plant Method for the initial separation of paclitaxel from branches and leaves" (publication number: CN1631084, publication date: June 29, 2005), "method for simultaneously extracting paclitaxel and 10-DABⅢ from branches and leaves of Taxus mandia" (publication number: CN102212045, Publication date: October 12, 2011), etc. Although these technologies can effectively separate and extract paclitaxel from the branches and leaves of Taxus chinensis, the purification effect is very unsatisfactory, and it cannot directly meet the medicinal standards (Chinese Pharmacopoeia 2010 edition). Subsequent purification operations will increase the extraction cost of paclitaxel, the extraction efficiency is low, and it is not suitable for large-scale batch production

Method used

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  • Method for extracting paclitaxel from taxus chinensis branch and leaf

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Experimental program
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Effect test

Embodiment 1

[0025] The present invention comprises the following steps:

[0026] 1). At room temperature, crush 1000kg of yew branches and leaves in 5m 3 Soak in methanol water for 10 hours, the concentration of methanol water is 80%; filter the soaking solution at a filtration rate of 1m 3 / h, about 23h when filtering;

[0027] 2). The filtrate obtained in step 1) is filtered and decolorized by an activated carbon column. The diameter of the activated carbon column is 790mm, and the weight of the activated carbon of the activated carbon column is 80kg;

[0028] 3). Concentrate the decolorized solution obtained in step 2) under reduced pressure, the temperature condition of the reduced pressure concentration is 70°C, and the volume is concentrated to 1.8m 3 , reclaiming methanol, the reclaimed methanol can be reused after blending; using chloroform to extract the product obtained by concentrating under reduced pressure 4 times, about 400L each time, and the extracts obtained by each ext...

Embodiment 2

[0040] The present invention comprises the following steps:

[0041] 1). At room temperature, crush 1000kg of yew branches and leaves in 5m 3 Soak in methanol water for 11 hours, the concentration of methanol water is 90%; filter the soaking solution at a filtration rate of 1.2m 3 / h, about 21h when filtering;

[0042] 2). The filtrate obtained in step 1) is filtered and decolorized with an activated carbon column. The diameter of the activated carbon column is 870mm, and the weight of the activated carbon of the activated carbon column is 55kg;

[0043] 3). Concentrate the decolorized liquid obtained in step 2) under reduced pressure. 3 , reclaiming methanol, the reclaimed methanol can be reused after blending; using chloroform to extract the product obtained by concentrating under reduced pressure 4 times, about 400L each time, and the extracts obtained by each extraction are combined;

[0044] 4). The extract obtained in step 3) is recovered under normal pressure at a te...

Embodiment 3

[0051] The present invention comprises the following steps:

[0052] 1). At room temperature, crush 1000kg of yew branches and leaves in 5m 3 Soak in methanol water for 12 hours, the concentration of methanol water is 75%; filter the soaking solution at a filtration rate of 0.8m 3 / h, the filter time is 25h;

[0053] 2). The filtrate obtained in step 1) is filtered and decolorized with an activated carbon column. The diameter of the activated carbon column is 800mm, and the weight of the activated carbon of the activated carbon column is 68kg;

[0054] 3). Concentrate the decolorized solution obtained in step 2) under reduced pressure. The temperature condition of the reduced-pressure concentration is 60°C, and the volume is concentrated to 1.2m 3 , reclaiming methanol, the reclaimed methanol can be reused after blending; using chloroform to extract the product obtained by concentrating under reduced pressure 4 times, about 400L each time, and the extracts obtained by each e...

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Abstract

The invention relates to a method for extracting paclitaxel from taxus chinensis branches and leaves, and the method comprises the following steps of: (1) soaking 1000 kg of pulverized taxus chinensis branches and leaves by using 5 m<3> of methanol, and filtering; (2) decoloring filter liquor; (3) decompressing and concentrating a decolored solution, and extracting; (4) degreasing and dewaxing extract liquor, crystallizing, depositing, filtering, and drying to obtain a primary product; (5) removing impurities contained in the primary product in a silicagel column, carrying out gradient elution, collecting paclitaxel-containing elution flows, and decompressing and concentrating to obtain a crude product; (6) stirring the crude product into silica gel, packing, carrying out gradient elution, collecting the paclitaxel-containing elution flows, and decompressing and concentrating to obtain a semi-finished product; (7) dissolving the semi-finished product, adding petroleum ether, standing, filtering, and drying to obtain a semi-finished product with the content more than or equal to 30%; (8) removing the impurities contained in the semi-finished product obtained from the step (7) in a silicagel column, carrying out gradient elution, collecting the paclitaxel-containing elution flows, and decompressing and concentrating to obtain a semi-finished product with the content more than or equal to 95%; and (9) dissolving the semi-finished product obtained from the step (8), filtering, adding normal hexane, standing, carrying out suction filtration; and drying to obtain a finished product with the content more than or equal to 99%.

Description

technical field [0001] The invention relates to a method for extracting natural organic compounds in plant branches and leaves, in particular to a method for extracting paclitaxel from yew branches and leaves. Background technique [0002] Paclitaxel is a compound extracted from the yew plant. It is mainly suitable for the treatment of ovarian cancer and breast cancer, as well as lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma, brain tumor, etc. One of the most effective new anti-cancer drugs, the total effective rate is over 75%. For a long time, paclitaxel has been extracted from the bark of yew. Because the bark of yew is a non-renewable resource, the raw material of paclitaxel is very limited; in addition, yew is recognized as an endangered natural rare anti-cancer drug in the world. Plants grow slowly under natural conditions and have poor regeneration ability. There is no large-scale yew raw material forest base in the world. China has listed ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
Inventor 赵家凡王昌全郑万奎
Owner SICHUAN XIANGGUANG AGRI TECH DEV
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