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A method for preparing paclitaxel extract by utilizing the waste residue of Taxus yunnanensis

A technology of paclitaxel and yew, applied in the direction of organic chemistry, etc., to achieve the effect of reducing production costs, fewer varieties, and reducing raw material costs

Active Publication Date: 2020-10-16
无锡紫杉药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, described method is only for the yew branches and leaves that do not extract

Method used

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  • A method for preparing paclitaxel extract by utilizing the waste residue of Taxus yunnanensis
  • A method for preparing paclitaxel extract by utilizing the waste residue of Taxus yunnanensis
  • A method for preparing paclitaxel extract by utilizing the waste residue of Taxus yunnanensis

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preparation example Construction

[0058] figure 1 It is a flow chart of the production process for extracting paclitaxel extract from Taxus yunnanensis branches and leaves waste residue provided by an embodiment of the present invention. The preparation method of the paclitaxel extract includes the following steps:

[0059] (1) According to the mass volume ratio of 1kg:(2~4.5)L, mix the waste residue of Taxus chinensis branches and leaves with a diameter not greater than 1cm and after extracting 10-deacetylbaccatin III with the extraction solvent, and heat it at 35° C. to 60° C. °C for 1-5 hours to obtain an extract solution with a temperature of 35-60 °C; wherein, the extraction solvent is a mixture of the first organic solvent and water, and the volume percentage of the first organic solvent is 70-95%. The first organic solvent is selected from any one or a combination of at least two of methanol, ethanol, and acetone;

[0060] (2) Concentrate the extract at a temperature of 35 to 60°C under reduced pressur...

Embodiment 1

[0064] A method for preparing paclitaxel extract by using the waste residue of Taxus yunnanensis branches and leaves, comprising the steps of:

[0065] (1) Get 3kg of branch and leaf waste residue (paclitaxel content 0.041wt%) of Taxus yunnanensis after extracting 10-deacetylbaccatin III, put the waste residue into a 50L extraction tank, add 80% (volume ratio) prepared 7.5 L of aqueous methanol solution was stirred and extracted, and the heating temperature of the extraction tank was set to 48°C. After reaching 48°C, it was continuously heated and stirred for 3 hours, and filtered to obtain 7.2L of paclitaxel extract;

[0066] (2) Put the paclitaxel extract into a 25L rotary evaporator to concentrate under reduced pressure, control the vacuum degree to -0.075~-0.095MPa, set the heating temperature to 45°C, and wait until the paclitaxel extract concentrate is concentrated to 1 / 3~1 of the original volume / 4 or so, detected with a density meter, the density of the concentrated so...

Embodiment 2

[0070] A method for preparing paclitaxel extract by using the waste residue of Taxus yunnanensis branches and leaves, comprising the steps of:

[0071] (1) Get the branch and leaf waste residue 50kg (paclitaxel content 0.043wt%) of Taxus yunnanensis, put the waste residue in a 500L extraction tank, add 150L of methanol aqueous solution of 83% (volume ratio) to carry out stirring extraction, and extract the tank heating temperature Set it to 45°C, continue heating and stirring for 2.5 hours after reaching 45°C, and filter to obtain 138L of paclitaxel extract;

[0072] (2) Put the paclitaxel extract into a 200L concentrator to concentrate under reduced pressure, control the vacuum degree to -0.075~-0.095MPa, set the heating temperature to 48°C, and wait until the paclitaxel extract concentrate is concentrated to 1 / 3~1 / 3 of the original volume 4 or so, detected with a density meter, the density of the concentrated solution is 0.98kg / L, and the concentrated solution is 28L;

[00...

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Abstract

The invention provides a method using taxus yunnanensis residues to prepare paclitaxel extract. The method comprises the following steps of (1) mixing an extracting solvent and the taxus yunnanensis residues, and extracting at the temperature of 35 to 60 DEG C, so as to obtain an extracting solution with temperature of 35 to 60 DEG C; (2) directly performing pressure-relief concentration on the extracting solution with temperature of 35 to 60 DEG C, so as to obtain a paclitaxel concentration solution; (3) extracting the paclitaxel concentration solution by a second organic solvent, so as to obtain a paclitaxel extracting solution; (4) performing pressure-relief concentration on the paclitaxel extracting solution, and performing pressure-relief drying, so as to obtain the paclitaxel extract. The method has the advantages that the recycling rate of paclitaxel is higher, and the content of paclitaxel in the paclitaxel extract is 1 to 3wt%; at least two types of solvents are used, and can be recycled, the environment-protection function is realized, and the cost is greatly reduced; the number of required steps is fewer, the operation is flexible, simple and convenient, and the method can be well applied into large-scale production.

Description

technical field [0001] The invention belongs to the technical field of resource recovery and utilization, and relates to the recycling of yew yunnanensis waste residue, in particular to a method for preparing paclitaxel extract from yew yunnanensis waste residue. Background technique [0002] Paclitaxel (Taxol) is the most promising anticancer drug discovered in the world in the past two decades. It was first isolated from the bark of Taxus brevifolia in 1967 and has been approved by the US FDA for ovarian cancer, breast cancer and non-cancerous drugs. Treatment of small cell lung cancer, etc. [0003] 10-Deacetylbaccatin III (10-DABIII) is a homologue of paclitaxel and is the main raw material for the synthesis of semi-synthetic paclitaxel and docetaxel. It also mainly exists in the branches, leaves, roots and bark of Taxus chinensis. With the gradual maturity of semi-synthetic technology, the method of extracting 10-DABIII from European yew (Taxus baccata) and then using ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/14
CPCC07D305/14
Inventor 任莉丁正飞胡立杨顺成喻琼林葛月兰
Owner 无锡紫杉药业股份有限公司