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Method of preparing five-alkaloid composition of corydalis saxicola bunting

The technology of alkaloid and composition is applied in the field of preparation of five kinds of alkaloid compositions of Coptidis chinensis, which can solve the problems of low total alkali content and poor water solubility, and achieve the effects of simple equipment, reduced toxic and side effects, and low cost.

Inactive Publication Date: 2008-05-07
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the common problem of the total alkaloid extract of Litectinus chinensis is that the content of total alkaloids is relatively low, and the water solubility is not good, so 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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Effect test

Embodiment 1

[0024] 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

[0026] 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

[0028] 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

A method for preparing a composition of five alkaloids of Litectin Rhizoma, comprising: (1) taking 1 part of crude extract of total alkaloids of Litectin Rhizoma Litectinus, refluxing and dissolving with 10-100 parts (V / W) of 75-100% ethanol solution , add 0.5-5 parts (W / W) of silica gel to mix the sample, stir and evaporate to dryness to obtain the mixed sample silica gel; (2) soak 6-20 parts (W / W) of silica gel in 5:1-1:1 ( V / V) of ethyl acetate and ethanol was applied to the column by wet method, and the mixed sample silica gel obtained in step (1) was added, and the gradient elution was performed with 3:1-1:1 (V / V) ethyl acetate and ethanol , collecting 1 / 1 of the eluate, concentrating and filtering to collect the filter cake, and drying to obtain the five alkaloid compositions of Litectin. The preparation method of the invention has the advantages of simple equipment, low cost, easy operation, short required time, high output 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. The following is the extract of Litectinum Rhizoma in the prior art [0003] Several preparation methods: [0004] The patent "purification of dehydrocarvitin from total alkaloids of Litectinus chinensis and injection preparation solubiliz...

Claims

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Application Information

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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
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