Method for separating paclitaxel and related taxane substances

A technology for taxanes and paclitaxel, which is applied in the field of efficient separation of taxol and related taxane substances, can solve the problems of high cost, poor separation efficiency and high solid-phase extraction separation efficiency, and achieves low production cost and wide range of raw materials. Effect

Inactive Publication Date: 2011-11-30
SHENYANG INSTITUTE OF CHEMICAL TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the methods for prepurifying paclitaxel and related analogues crude products reported in the literature mainly include: organic solvent extraction, solid phase column extraction, etc. Among them, organic solvent extraction has poor separation efficiency, high toxicity, and high cost, and solid phase extraction High efficiency, but small processing volume and high cost

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Stir and mix 15 g D101 resin and 15 g NKA-2 resin in a beaker, and put them into a glass column. Weigh 1.0 g of yew leaf extract extract, add 10 mL of absolute ethanol and stir to dissolve. Add 5 g of D3520 resin weighed into the sample solution for stirring and adsorption, and put it into the top of the packed column after the solvent is evaporated to dryness. After equilibrating the packed column with deionized water, gradient elution was performed with 300 mL 35% ethanol solution, 300 mL 45% ethanol solution and 300 mL 55% ethanol solution in sequence. The above eluate was concentrated under reduced pressure, the solvent was recovered, and crude products rich in 10-deacetylbaccatin, 10-deacetyl-7-xylose-paclitaxel and paclitaxel were obtained after vacuum drying at 80 °C.

Embodiment 2

[0024] Stir and mix 20 g DA-201 resin and 5 g AB-8 resin in a beaker, and put them into a glass column. Weigh 1.5 g of yew branches and leaves extract, add 9 mL of acetone and stir to dissolve. The above sample solution was stirred and adsorbed with 8 g of silica gel, and loaded into a packed column after the solvent was evaporated to dryness. After equilibrating the packed column with deionized water, gradient elution was performed with 350 mL 40% acetone solution, 350 mL 50% acetone solution and 350 mL 60% acetone solution in sequence. The above eluate was concentrated under reduced pressure to recover the solvent, and after vacuum drying at 80°C, crude products rich in 10-deacetylbaccatin, 10-deacetyl-7-xylose-paclitaxel and paclitaxel were obtained respectively.

Embodiment 3

[0026] Stir and mix 30 g D3520 resin and 45 g X-5 resin in a beaker, and put them into a glass column. Weigh 5 g of yew leaf extract extract, add 25 mL of ethanol and stir to dissolve. Add 5 g of diatomaceous earth to adsorb the sample solution under stirring, and put it on the top of the packed column after the solvent is evaporated to dryness. After equilibrating the packed column with deionized water, gradient elution was performed with 900 mL 35% acetonitrile solution, 900 mL 45% acetonitrile solution and 900 mL 55% acetonitrile solution in sequence. The above eluents were concentrated under reduced pressure to recover the solvent, and vacuum-dried at 80°C to obtain crude products rich in 10-deacetylbaccatin, 10-deacetyl-7-xylose-paclitaxel and paclitaxel.

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PUM

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Abstract

The invention discloses a method for separating paclitaxel and related taxane substances, and belongs to a technical method for chemically separating natural products and forest products. The method is characterized by comprising the following steps of: (1) uniformly mixing two kinds of macroporous resin in a certain mass ratio, and loading in a glass column to obtain a mixed resin packed column; and (2) dissolving a crude extract of taxus chinensis in a solvent in a ratio of 1:5 with stirring, adding an adsorbent, stirring until the solvent is completely volatilized, loading in the top end of the packed column, adding a gradient eluent for elution, collecting fractions in various gradients, and concentrating to obtain the paclitaxel and related taxane substances, which have obviously improved content. The raw materials used in the method are wide in range, and various crude extracts containing the paclitaxel and related taxane substances can be separated; the resin is commercially common resin, cheap and readily available; and the solvent is a common solvent which is low in toxicity and easy to recover. The production cost is low.

Description

technical field [0001] The invention belongs to natural products and forest product chemical separation technology methods, in particular to a method for efficiently separating paclitaxel and related taxanes. Background technique [0002] Paclitaxel is a complex secondary metabolite present in yew plants. It has been clinically shown that paclitaxel has significant anti-tumor effects on various cancers including ovarian cancer and breast cancer. Different from the mechanism of action of vinblastine and colchicine, paclitaxel is the only drug known to promote microtubule polymerization and stabilize the polymerized microtubules. [0003] The content of paclitaxel in the yew plant is very low, only a few parts per hundred thousand to a few parts per ten thousand. Therefore, to extract the crude taxol from plants to clinical application, it needs to be separated and purified through complicated processes. The separation and purification process of paclitaxel mainly includes ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
Inventor 陈家祥聂宁马婧舒
Owner SHENYANG INSTITUTE OF CHEMICAL TECHNOLOGY
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