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Method of preparing five-alkaloid composition of corydalis saxicola bunting

A technology of alkaloids and compositions, which is applied in the field of preparation of five alkaloid compositions of Litectinus chinensis, can solve the problems of poor water solubility and low total alkali content, and achieve the effects of reducing toxic and side effects, simple equipment, and easy operation

Inactive Publication Date: 2010-08-18
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, the common problem of the total alkaloid extract of Litectinus chinensis is that the content of total alkaloids is relatively low, the water solubility is not good, and more solubilizers need to be added, which is not completely consistent with the principle of "careful selection" of solubilizers for intravenous injections.

Method used

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  • Method of preparing five-alkaloid composition of corydalis saxicola bunting
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  • Method of preparing five-alkaloid composition of corydalis saxicola bunting

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Experimental program
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Effect test

Embodiment 1

[0023] Take 2.0g of the crude extract of total alkaloids of Litectinus chinensis, add 200ml of 75% ethanol, heat to reflux for 1 hour, filter while it is hot, add 2.0g of silica gel to the filtrate, stir and evaporate to dryness, and then get the mixed sample silica gel; take 12g of silica gel with ethyl acetate After soaking in ester: ethanol (3:1), put it on the column by wet method, fill the sample silica gel on the top of the column, carry out gradient elution with ethyl acetate: ethanol (3:1-1:1), and collect the 1:1 fraction The eluate is concentrated, cooled, filtered, and the filter cake is collected and dried to obtain the composition of the five alkaloids of the rhizome. The five alkaloids are dehydrosteiner's corydine, dehydroisoaporcarvetin, dehydroapporcavetin, coptisine and dehydrocarvetin. The total amount of the five alkaloids is 87%.

Embodiment 2

[0025] Take 2.0g of the crude extract of total alkaloids of Litectinus chinensis, add 80ml of 80% ethanol, heat and reflux for 1 hour, filter while it is hot, add 1.0g of silica gel to the filtrate, stir and evaporate to dryness, and then get the mixed sample silica gel; take 20g of silica gel with ethyl acetate After soaking in ester: ethanol (5:1), put it on the column by wet method, fill the sample silica gel on the top of the column, carry out gradient elution with ethyl acetate: ethanol (3:1-1:1), and collect the 1:1 fraction The eluate is concentrated, cooled, filtered, and the filter cake is collected and dried to obtain the composition of the five alkaloids of the rhizome. The five alkaloids are dehydrosteiner's corydine, dehydroisoaporcarvetin, dehydroapporcavetin, coptisine and dehydrocarvetin. The total amount of the five alkaloids is 92%.

Embodiment 3

[0027] Take 2.0g of the crude extract of total alkaloids of Litectinus chinensis, add 60ml of 90% ethanol, heat and reflux for 1 hour, filter while it is hot, add 4.0g of silica gel to the filtrate, stir and evaporate to dryness, and then get the mixed sample silica gel; take 16g of silica gel with ethyl acetate After soaking in ester: ethanol (1:1), put it on the column by wet method, fill the sample silica gel on the top of the column, carry out gradient elution with ethyl acetate: ethanol (3:1-1:1), and collect the 1:1 fraction The eluate is concentrated, cooled, filtered, and the filter cake is collected and dried to obtain the composition of the five alkaloids of the rhizome. The five alkaloids are dehydrosteiner's corydine, dehydroisoaporcarvetin, dehydroapporcavetin, coptisine and dehydrocarvetin. The total amount of the five alkaloids is 95%.

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Abstract

The invention relates to a preparation method for corydalis saxicola bunting five-alkaloid compound. The method comprises the steps as follow: (1) one proportion of corydalis saxicola bunting total alkaloid crude extract is prepared and back-flew and dissolved through 10 to 100 parts (V / W) of ethanol solution with concentration of 75 to 100 percent, and 0.5 to 5 parts (W / W) of silica gel mixed sample is added into the solution, and the solution is then mixed and steamed out so as to obtain mixed sample silica gel; (2) 6 to 20 parts (W / W) of silica gel are dipped in 5:1 to 1:1 (V / V) of ethyl acetate and ethanol, and then are poured into a column in a wet way, and the mixed sample silica gel obtained from step (1) is added in, and then is processed through gradient elution with 3:1 to 1:1 (V / V) of ethyl acetate and ethanol; part of 1 / 1 elution liquid is collected, and then the filtered residues are collected after condensing and filtering the liquid; and the corydalis saxicola bunting five-alkaloid compound is obtained by drying the filter residues. The invention has the advantages of simple device, low cost, easy operation, short time taken, high yield and high safety.

Description

technical field [0001] The invention relates to a preparation method of a composition of five alkaloids of Litrichum chinensis. Background technique [0002] Corydalis saxicola Bunting has a good therapeutic effect on viral hepatitis, liver fibrosis, etc., and its effective parts are alkaloids, of which the five main alkaloids are dehydrosteen's corydine, dehydroisoaporca Vidin, dehydroaporcavitin, coptisine, and dehydrocarvetin. Many clinical observations show that Yanhuanglian injection has good clinical application prospects in the treatment of acute and chronic hepatitis, and most of them are clinical empirical treatments: dilute Yanhuanglian injection with 10% or 5% glucose injection (use Tween 80 as a solubilizer) after dripping. Below are several preparation methods of Litectin Rhizoma extract in the prior art: [0003] The patent "purification of dehydrocarvitin from total alkaloids of Litectinus chinensis and injection preparation solubilization method" (applicat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61K31/4375A61K36/66A61P31/12A61P1/16
Inventor 陈满仓奉建芳刘小叶祝林邹凌燕
Owner SHANGHAI INST OF PHARMA IND CO LTD