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Extracting method of high-purity taxol and derivative thereof

An extraction method, paclitaxel technology, applied in the direction of drug combination, medical raw materials derived from gymnosperms, anti-tumor drugs, etc., can solve the problems of high cost, large loss of components, low level of industrialization, etc., and achieve low cost of use and high composition The effect of less loss and complete extraction

Inactive Publication Date: 2010-10-27
张鹏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the extraction and separation of paclitaxel from the branches and leaves of Taxus mandia also has unique difficulties: the content of pigments, waxes, and tannins in the branches and leaves is higher than that in the bark, and it is more difficult to deal with impurities; it is speculated that the taxol bond It may be a special form of paclitaxel transported in plants. It is generally believed that the synthetic parts of paclitaxel are buds, branches and leaves or roots, stems, etc., and the storage part is bark. Therefore, the whole plant of Taxus mandia Extraction of paclitaxel will lose more conjugated paclitaxel
[0008] Therefore, the current main methods for extracting paclitaxel and its derivatives from the branches and leaves of Taxus mandia have shortcomings such as low extraction efficiency, large loss of components, high cost, and low industrialization level, especially paclitaxel in the dry paste of paclitaxel extract. The content is very low, the content of paclitaxel derivatives is lower, and the impurities are high, which has caused great difficulties for the subsequent purification and separation of paclitaxel and pure paclitaxel derivatives

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Take appropriate amount of branches and leaves of Taxus chinensis, vacuum-dry at 40°C, and measure the water content as 8.5% by the loss-on-drying method. Grind the dried yew branches and leaves into 100-mesh powder, weigh 200g, put it in a cloth bag, add 2000mL of methanol, let it stand overnight (about 15 hours), heat to 40°C and reflux for 3.5 hours, after natural cooling, Filter to obtain filter residue 1, and recover methanol from the filtrate under reduced pressure to obtain concentrated solution 1. Add 1600 mL of methanol to the filter residue 1, reflux and extract at 40°C for 3 hours, let stand overnight (about 15 hours), and filter to obtain the filter residue 2, and recover the methanol from the filtrate under reduced pressure to obtain the concentrate 2. The filter residue 2 was percolated and extracted with 1600 mL of methanol, and the percolated solution was decompressed to recover methanol to obtain the concentrated solution 3. Combine Concentrate 1, Conc...

Embodiment 2

[0027] Take an appropriate amount of twigs and leaves of Taxus chinensis, dry in the shade, and measure the water content as 9.2% by the weight loss on drying method. Grind the dried yew branches and leaves into 100-mesh powder, weigh 5kg, put it in a cloth bag, add 50L of methanol, leave it overnight (about 15 hours), heat to 40°C for reflux extraction for 3.5 hours, after natural cooling, Filter to obtain filter residue 1, and recover methanol from the filtrate under reduced pressure to obtain concentrated solution 1. Add 40L of methanol to the filter residue 1, reflux and extract at 40°C for 3.5 hours, let stand overnight (about 15 hours), filter to obtain filter residue 2, and recover methanol from the filtrate under reduced pressure to obtain concentrate 2. The filter residue 2 was percolated and extracted with 40 L of methanol, and the percolated solution was decompressed to recover methanol to obtain the concentrated solution 3. Combine concentrated solution 1, concent...

Embodiment 3

[0029] An appropriate amount of twigs and leaves of Taxus chinensis were dried at 40°C, and the water content was 9.1% as measured by the drying weight loss method. Grind the dried yew branches and leaves into 100-mesh powder, weigh 200kg, put it in a cloth bag, add 2000L methanol, let it stand overnight (about 15 hours), heat it to 40°C for reflux extraction for 3 hours, and cool it naturally. Filter to obtain filter residue 1, and recover methanol from the filtrate under reduced pressure to obtain concentrated solution 1. Add 1600L methanol to the filter residue 1, reflux and extract at 40°C for 4 hours, let stand overnight (about 15 hours), filter to obtain filter residue 2, and recover methanol from the filtrate under reduced pressure to obtain concentrate 2. The filter residue 2 was percolated and extracted with 1600L of methanol, and the percolated solution was decompressed to recover methanol to obtain the concentrated solution 3. Combine concentrated solution 1, conce...

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Abstract

The invention relates to an extracting method of a high-purity taxol and a derivative thereof, in particular to a method for extracting the high-purity taxol and the derivative thereof from Taxus Media branches and leaves, which comprises the steps of drying and grinding the Taxus Media branches and leaves, extracting with carbinol for three times, respectively decompressing the three extracted liquids and combining after recovering the carbinol, degreasing respectively with isometric petroleum ether (60-90 DEG C) and normal hexane and drying into dry paste at the temperature of not more than 50 DEG C. The extraction method has the advantages of complete extraction of the taxol and the derivative thereof, high purity and fewer impurities, and creates more favorable conditions for the follow-up industrialized or non industrialized purification and separation of medicines of taxol and derivative thereof.

Description

technical field [0001] The invention belongs to the technical field of extraction of natural chemical substances, in particular to a method for extracting paclitaxel and derivatives thereof, in particular to a method for extracting high-purity paclitaxel and derivatives thereof from branches and leaves of Taxus chinensis. Background technique [0002] Paclitaxel and paclitaxel injection have been recorded in the current United States Pharmacopoeia and Chinese National Drug Standards, and are used for the treatment of metastatic ovarian cancer, breast cancer, lung cancer, and esophageal cancer. Paclitaxel, English name Paclitaxel, molecular formula C 47 h 51 NO 14 , Molecular weight 853.92, white crystalline powder, odorless, tasteless, the United States Pharmacopoeia and China National Drug Standards stipulate that its purity requirement is calculated as dry product, containing C 47 h 51 NO 14 It should be 98.0% to 102.0%. [0003] Paclitaxel is one of the hottest new ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/13A61P35/00C07D305/14A61K135/00A61K127/00
Inventor 张鹏
Owner 张鹏
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