Method for extracting paclitaxel from taxus chinensis

A technology of paclitaxel and yew, which is applied in the field of extracting paclitaxel from yew, can solve the problems of complicated steps in the separation process, low yield of paclitaxel at one time, and high toxicity of the eluent, and achieve low separation cost, strong innovation, and high product yield. big effect

Inactive Publication Date: 2020-02-28
普洱大华林业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The steps of the separation process are cumbersome, and the yield of paclitaxel with a purity of more than 99% is low
Solvents, eluents, etc. are highly toxic, causing serious pollution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A method for extracting paclitaxel from Chinese yew, comprising the steps of:

[0035] (1) Prepare the ammonium nitrate solution D1 with a concentration of 15% in purified water, adjust the pH value to 6.0 ± 0.2, add methanol (≥98%) and mix to make a mixed solution M1, for subsequent use: in the M1, by volume ratio, D1: Methanol = 1:4;

[0036] (2) Dry and pulverize the yew bark or branches and leaves to 80-90 mesh, add solution M1 twice its mass, and carry out leaching for 3 times, each time the extract is stirred and leached for 2 hours, and then removed by pressure filtration For the residue, add the filtrate to the extraction phase M2 (by volume ratio, ethyl acetate: acetone = 1:1) whose volume is 0.8 times, stir for 0.5 hours, and let stand;

[0037] (3) After completely stratifying, remove the lower impurity part and leave the upper oil phase solution;

[0038] (4) Collect the upper layer oil phase solution, concentrate under reduced pressure at 50° C., stop con...

Embodiment 2

[0047] A method for extracting paclitaxel from Chinese yew, comprising the steps of:

[0048] (1) Prepare the ammonium nitrate solution D1 with a concentration of 20% in purified water, adjust the pH value to 6.0 ± 0.2, add methanol (≥98%) and mix to make a mixed solution M1, for subsequent use: in the M1, by volume ratio, D1: Methanol = 1:4;

[0049] (2) Dry and crush the yew bark or branches and leaves to 80-90 mesh, add solution M1 with 4 times its mass, and carry out leaching 4 times, each time the extract is stirred and leached for 4 hours, and then removed by pressure filtration For the residue, add the filtrate to the extract phase M2 (according to the volume ratio, ethyl acetate: acetone = 1:1) whose volume is 1.2 times, stir for 2 hours, and let stand;

[0050] (3) After completely stratifying, remove the lower impurity part and leave the upper oil phase solution;

[0051] (4) Collect the upper layer oil phase solution, concentrate under reduced pressure at 55° C., ...

Embodiment 3

[0059] A method for extracting paclitaxel from Chinese yew, comprising the steps of:

[0060] (1) Prepare the ammonium nitrate solution D1 with a concentration of 18% with pure water, adjust the pH value to 6.0 ± 0.2, add methanol (≥98%) and mix to make a mixed solution M1, for subsequent use: in the M1, by volume ratio, D1: Methanol = 1:4;

[0061](2) Dry and crush the bark or branches and leaves of yew to 80-90 mesh, add solution M1 with 3 times its mass, and carry out leaching 4 times, each time the extract is stirred and leached for 3 hours, and then removed by pressure filtration For the residue, add the filtrate to the extraction phase M2 (according to the volume ratio, ethyl acetate: acetone = 1:1), stir for 1.2 hours, and let stand;

[0062] (3) After completely stratifying, remove the lower impurity part and leave the upper oil phase solution;

[0063] (4) Collect the upper layer oil phase solution, concentrate under reduced pressure at 52°C, stop concentrating when...

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PUM

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Abstract

The invention provides a method for extracting paclitaxel from taxus chinensis. The method comprises the following steps: compounding an ammonium nitrate solution and methanol to prepare a mixed solution M1; adding the tissue of taxus chinensis plants into the solution M1, stirring, leaching, carrying out filter pressing to remove dregs, adding an obtained filtrate into an extraction phase M2 (ethyl acetate: acetone = 1: 1), stirring, and standing; after complete layering, removing a lower impurity part, and reserving an upper layer oil phase solution; collecting an upper layer oil phase solution, concentrating under reduced pressure, adding reverse extraction phase solvent petroleum ether into an obtained concentrated solution, generating flocculent precipitate after petroleum ether is added, centrifuging to remove the solvent, and collecting an obtained precipitate; and carrying out silica gel column chromatography purification twice to obtain a paclitaxel crude product, and finally,carrying out reversed-phase high-pressure liquid chromatographic separation to obtain high-purity paclitaxel with the purity of 99.6% or above. The method is simple in process and low in cost, the solvent and the eluent can be recycled, the method is suitable for industrial production, and plant resources are protected.

Description

technical field [0001] The invention relates to the technical field of medicine extraction, in particular to a method for extracting paclitaxel from yew. Background technique [0002] Paclitaxel, English name Paclitaxel, alias taxol, porphyrin, special element, chemical name 5β, 20-epoxy-1, 2α, 4, 7β, 10β, 13α-hexahydroxytaxane-11-en-9-one -4,10-diacetate-2-benzoate-13[(2'R,3'S)-N-benzoyl-3-phenylisoserine ester], molecular weight 853.92, molecular formula C47H51NO14. It is a complex secondary metabolite in the Taxus genus, and it is the only drug known to promote microtubule polymerization and stabilize the polymerized microtubules. Paclitaxel is currently mainly used in the treatment of ovarian cancer and breast cancer, and has a certain effect on lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma and brain tumor. Therefore, the production of paclitaxel API has broad market prospects. [0003] For the separation and purification of Taxus paclitaxel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
CPCC07D305/14
Inventor 李福荣岑德誉李坤
Owner 普洱大华林业科技有限公司
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