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Process for preparing vinblastine

A technique for vinblastine and periwinkle, which is applied in the field of vinblastine preparation, can solve problems such as unfavorable industrialization, large equipment investment, environmental pollution and the like, and achieves the effects of simple operation, small equipment investment and less pollution

Inactive Publication Date: 2010-02-10
SUZHOU PAITENG BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, solvent method and supercritical extraction method are mainly used to extract vinblastine. The former uses a large amount of organic solvents, which pollutes the environment; the latter has a large investment in equipment, which is not conducive to industrialization

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Take 1Kg of the whole periwinkle plant, soak it in 8 times the volume of 5% acetic acid aqueous solution for 2 hours, microwave-assisted extraction, extraction power 600W, extraction time 2 minutes, filter, adjust the pH of the filtrate to 8 with ammonia water, use H-1020 Adsorbed on a macroporous adsorption resin column, eluted with 20% ethanol with pH=5 to remove impurities, then eluted with 95% ethanol, concentrated the eluate, added acetone to crystallize, washed and dried to obtain 0.36g of vinblastine, which was obtained by HPLC Detection, its purity is 97.6%.

Embodiment 2

[0016] Take 1Kg of the whole periwinkle plant, soak it with 12 times the concentration of 20% acetic acid aqueous solution for 2 hours, microwave-assisted extraction, extraction power 600W, extraction time 8 minutes, filter, adjust the pH of the filtrate to 8 with ammonia water, use X-5 Adsorbed on a macroporous adsorption resin column, eluted with 60% ethanol with pH = 5 to remove impurities, then eluted with 95% ethanol, concentrated the eluate, added acetone to crystallize, washed and dried to obtain vinblastine 0.48g, and used HPLC Detection, its purity is 96.7%.

Embodiment 3

[0018] Take 1Kg of the whole periwinkle plant, soak it with 10 times the volume of 10% acetic acid aqueous solution for 2 hours, microwave-assisted extraction, extraction power 600W, extraction time 4 minutes, filter, and adjust the pH of the filtrate to 8 with ammonia water, using AB-8 Adsorbed on a macroporous adsorption resin column, eluted with 50% ethanol with pH=5 to remove impurities, then eluted with 95% ethanol, concentrated the eluate, added acetone to crystallize, washed and dried to obtain 0.42g of vinblastine, and used HPLC Detection, its purity is 98.9%.

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PUM

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Abstract

The invention relates to a process for preparing vinblastine, which has simple and convenient operation and less pollution and equipment investment. The process comprises the following steps: soakingthe whole catharanthus roseus by 8-12 times of acetic acid aqueous solution with concentration of 5-20 percent for 2 hours; assisting to extract by a microwave with the extracting power of 600W and the extracting time of 2-8 minutes; filtering and adjusting the pH value of filter liquor to 8 by ammonia water; adsorbing by a macroporous absorption resin column; eluting and removing impurities by 20-60 percent of alcohol with the pH value being equal to 5; eluting by 95 percent of alcohol; concentrating eluent, adding acetone crystals, washing and drying to obtain the vinblastine. The process for preparing the vinblastine is easy to realize industrialization amplification.

Description

technical field [0001] The invention relates to a method for preparing vinblastine, in particular to a method for extracting vinblastine from periwinkle flowers. Background technique [0002] Vinblastine (vinblastine) is a dipolyindole alkaloid with obvious antitumor activity extracted from the plant Vinca of Apocynaceae. It has significant curative effect on Hodgkin's disease, non-small cell lung cancer and malignant lymphoma. Its sulfate has been widely used clinically for more than 30 years, and is still one of the main tumor drugs so far. Since Beer and Johnson discovered and extracted vinblastine from periwinkle in the middle and late 1950s, more than 100 indole alkaloids have been isolated from 1Kg of the whole plant of periwinkle, and the content of vinblastine is about 4 / 100,000. At present, vinblastine is mainly extracted from natural plants. Although vinblastine and its derivatives can be obtained by chemical synthesis and semi-synthetic methods, there are also s...

Claims

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Application Information

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IPC IPC(8): C07D519/04
Inventor 王琳范淦彬
Owner SUZHOU PAITENG BIOLOGICAL MEDICAL TECH
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