Galantamin hydrobromide production method

A technology of galantamine hydrobromide and galantamine, applied in the direction of fermentation, etc., can solve the problems of incompatibility with high-quality requirements, low yield, and low galantamine content

Inactive Publication Date: 2008-06-11
贵州芊芊园艺新技术发展公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The content of galantamine in Amaryllidaceae Amaryllidaceae plants is very low, only 1 / 10,000 to 3, and there are many types of other alkaloids, so it is very difficult to extract and separate high-purity galantamine. Solvent extraction separation process, low yield, poor purity, long cycle, difficult to remove impurities similar to alkaloids, does not meet the current high-quality requirements of galantamine in various countries in the world, and there is an urgent need for a stable high-purity galantamine Production Process

Method used

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  • Galantamin hydrobromide production method

Examples

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Effect test

Embodiment 1

[0066] Example 1. Add 200 kg of lycoris powder crushed to 80 meshes into the extraction equipment, add 800 kg of water, add 400 g of medium-temperature amylase, and hydrolyze it at 60°C for 2 hours to obtain a biochemical solution. Adjust the biochemical solution with 10% sodium hydroxide solution When the pH reaches 10, use a mixed solvent of petroleum ether ethyl acetate (petroleum ether: ethyl acetate = 9:1) to continuously and dynamically countercurrently extract the biochemical liquid until there is no galantamine in the extraction liquid at the overflow port of the extraction equipment, then concentrate and recover the solvent , 5 L of concentrated solution was obtained. Use 5L of 2% HCl solution to extract the concentrated solution for 5 times to obtain the stripping acid solution, add 10% NaOH to adjust the pH of the stripping acid solution to 10, use 25L ethyl acetate to extract the stripping acid solution for 5 times, and obtain the ethyl acetate extraction solution ...

Embodiment 2

[0067] Example 2: Add 200 kg of lycoris powder crushed to 80 meshes into the extraction equipment, add 1000 kg of water, add 500 g of medium-temperature amylase, and hydrolyze it at 60°C for 2 hours to obtain a biochemical solution, adjust the pH of the biochemical solution to 11 with 10% NaOH, and use Petroleum ether ethyl acetate (petroleum ether: ethyl acetate = 8: 2) mixed solvent for continuous dynamic countercurrent extraction of biochemical liquid until the extraction liquid at the overflow port of the extraction equipment has no galantamine, concentrate and recover the solvent to obtain 5.5 L of concentrated liquid . Use 5.5L of 5% HCL solution to extract the concentrated solution 5 times to obtain the stripping acid solution, add 10% NaOH to adjust the pH of the stripping acid solution to 10, extract with 30L ethyl acetate, and concentrate the ethyl acetate extract to dryness under reduced pressure to obtain 140 g of total alkaloids contained lycorine, saffronine, hom...

Embodiment 3

[0068] Example 3: Add 200 kg of lycoris powder crushed to 80 mesh in the extraction equipment, add 1200 kg of water, add 400 g of medium-temperature amylase, and hydrolyze it at 60°C for 2 hours to obtain a biochemical solution, adjust the pH to 10-11 with 10% NaOH, and use Petroleum ether ethyl acetate (petroleum ether: ethyl acetate = 9:1) mixed solvent for continuous dynamic countercurrent extraction of the biochemical liquid until the extraction liquid at the overflow port of the extraction equipment was free of galantamine, concentrated and recovered the solvent to obtain 6 L of concentrated liquid. Use 6L of 5% HCL solution to extract the concentrated solution for 5 times to obtain the stripping acid solution, add 10% NaOH to adjust the pH of the stripping acid solution to 10-11, extract the stripping acid solution with 30L ethyl acetate to obtain the ethyl acetate extract , the ethyl acetate extract was concentrated to dryness under reduced pressure to obtain 120 g of to...

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Abstract

The invention discloses a galantamin hydrobromide producing method for treating senile dementia, which comprises the following steps: adopting the method of enzyme reaction, continuous kinesis flow upstream extracting and column chromatography to extract galantamin with purity of 99% from Amaryllidaceae plant; Using galantamin with purity of 99 percent as raw material; obtaining galantamin hydrobromide with purity of 98.5. percent. The invention discloses an extracting galantamin of purity at 99% process flow and technological condition from Amaryllidaceae plant, which adapts for industrialization production.

Description

Technical field: [0001] The invention relates to a production method of a medicine, in particular to a production method of galanthamine hydrobromide, a drug with good curative effect for treating senile dementia. Background technique: [0002] Galanthamine hydrobromide English name: Galanthamine Hydrobromide, scientific name: 11-methyl-3-methoxy-4a, 5, 9, 10, 11, 12-hexahydro-benzofuran (3a, 3, 3 -ef)-(2) azepine-6-alcohol hydrobromide; , the molecular formula is C 17 h 21 o 3 N·HBr, its characteristic is white or almost white crystalline powder, odorless, bitter taste, this product is soluble in water, slightly soluble in ethanol, insoluble in acetone, chloroform, ether or benzene. Galantamine hydrobromide is a second-generation acetylcholinesterase inhibitor, and it is a reversible acetylcholinesterase inhibitor, which can resist acetylcholinesterase and regulate pharyngeal acid receptors. This product can improve the conduction between nerves and muscles, and is used...

Claims

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Application Information

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IPC IPC(8): C12P17/18
Inventor 黄玉君周玉梁世康杨航曹永文
Owner 贵州芊芊园艺新技术发展公司
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