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Method for efficiently extracting camptothecin derivative

A technology for camptothecin and derivatives, which is applied in the field of efficient extraction of camptothecin derivatives, can solve the problems of being unable to put into industrial production, backward production technology, and large waste of resources, so as to increase equipment utilization, reduce equipment investment, and improve The effect of production efficiency

Inactive Publication Date: 2011-06-15
NORTHEAST FORESTRY UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because camptothecin and 10-hydroxycamptothecin have unique anti-tumor effects naturally, in recent years, the demand for camptothecin and 10-hydroxycamptothecin in the international pharmaceutical mainstream market has risen sharply, but the existing extraction Low technical yield and large waste of resources have seriously restricted the development of camptothecin and 10-hydroxycamptothecin pharmaceutical industry
[0003] The total synthesis of camptothecin and the artificial semi-synthetic method using camptothecin as the parent compound to obtain 10-hydroxycamptothecin have been successful, but due to the long route, low yield and high production cost, it cannot be put into industrial production
Therefore, the use of modern technology to extract and separate camptothecin derivatives and increase the production of camptothecin derivatives has become a hot spot in current research. However, the current production process for extracting camptothecin derivatives is backward and costly, and has become an anti-camptothecin derivative. Bottleneck in cancer drug development

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] 1 Camptothecin contains a large amount of oil components. Before extracting camptothecin and 10-hydroxycamptothecin, supercritical fluid CO 2 Extract the magma fruit to remove oil, the extraction pressure is 30MPa, the extraction temperature is 45°C, the extraction time is 3.5h, the separation pressure is 8-12MPa, and the separation temperature is 25-35°C.

[0013] 2. Take degreased symphylla fruit and dried symphylla leaves as raw materials, mix and homogenate to extract two kinds of alkaloids, the mixing ratio of the two raw materials is 1:2.6, the homogenate solvent is 65% ethanol, and the ratio of solid to liquid is 1:12 , Homogenization time is 6.5min. Then adopt the negative pressure cavitation mixing method to extract camptothecin and 10-hydroxycamptothecin in the homogenate solids, use 55% ethanol as the extraction solvent, the ratio of solid to liquid is 1: 15, the ventilation rate is 70L / min, and the negative pressure cavitation Extract for 25min.

[0014] 3...

Embodiment 2

[0019] 1 Camptothecin contains a large amount of oil components. Before extracting camptothecin and 10-hydroxycamptothecin, supercritical fluid CO 2 Extract the symphylla fruit to remove oil, the extraction pressure is 33MPa, the extraction temperature is 40°C, the extraction time is 4.0h, the separation pressure is 8-12MPa, and the separation temperature is 25-35°C.

[0020] 2. Take degreased symphylla fruit and dried symphylla leaves as raw materials, mix and homogenate to extract two kinds of alkaloids, the mixing ratio of the two raw materials is 1:3, the homogenate solvent is 60% ethanol, and the ratio of solid to liquid is 1:15 , The homogenization time is 7.0min. Then adopt the negative pressure cavitation mixing method to extract camptothecin and 10-hydroxycamptothecin in the homogenate solid, use 60% ethanol as the extraction solvent, the ratio of solid to liquid is 1: 12, the ventilation rate is 75L / min, and the negative pressure cavitation Extract for 20min.

[00...

Embodiment 3

[0026] 1 Camptothecin contains a large amount of oil components. Before extracting camptothecin and 10-hydroxycamptothecin, supercritical fluid CO 2 Extract the haptoki fruit to remove oil, the extraction pressure is 35MPa, the extraction temperature is 45°C, the extraction time is 4.5h, the separation pressure is 8-12MPa, and the separation temperature is 25-35°C.

[0027] 2. Take degreased symphylla fruit and dried symphylla leaves as raw materials, mix and homogenize to extract two alkaloids, the mixing ratio of the two raw materials is 1:4, the homogenate solvent is 70% ethanol, and the ratio of solid to liquid is 1:18 , Homogenization time is 7.5min. Then adopt the negative pressure cavitation mixing method to extract camptothecin and 10-hydroxycamptothecin in the homogenate solid, use 65% ethanol as the extraction solvent, the ratio of solid to liquid is 1: 14, the ventilation rate is 80L / min, and the negative pressure cavitation Extract for 30min.

[0028] 3. Take the...

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Abstract

The invention relates to a method for efficiently extracting a camptothecin derivative. The method comprises the following steps of: mixing degreased common camptotheca fruits and dried common camptotheca leaves, homogenating and extracting; and freshly grinding, mixing and homogenating common camptotheca seed buds and fresh common camptotheca leaves according to a stress biology principle so as to improve the output of the camptothecin derivative in the raw materials. On the basis of the method, a new high-efficiency extracting and purifying process of camptothecin and 10-hydroxy camptothecin is obtained through applying serial innovation researches of negative-pressure cavitation mixed rotating high-efficiency strengthened leaching, negative-pressure cavitation liquid-liquid mixed rotating extracting, recrystallizing, preparation type HPLC(High Performance Liquid Chromatography) refining, and the like.

Description

Technical field: [0001] The invention relates to a method for efficiently extracting camptothecin derivatives. Background technique: [0002] Since entering the 21st century, cancer has become a major hidden danger to human health, seriously threatening human health. Because camptothecin and 10-hydroxycamptothecin have unique anti-tumor effects naturally, in recent years, the demand for camptothecin and 10-hydroxycamptothecin in the international pharmaceutical mainstream market has risen sharply, but the existing extraction The technical yield is low and the waste of resources is large, thereby seriously restricting the development of the pharmaceutical industry of camptothecin and 10-hydroxycamptothecin. [0003] The total synthesis of camptothecin and the artificial semi-synthesis of 10-hydroxycamptothecin using camptothecin as the parent compound have been successful, but due to the long route, low yield and high production cost, it cannot be put into industrial product...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/22
Inventor 祖元刚史伟国杨磊祖柏实赵春建李庆勇
Owner NORTHEAST FORESTRY UNIVERSITY
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