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Extracting process for bilobalide A, B, C and its preparation

A technology of ginkgolide and extraction process, which is applied in the field of extraction of effective parts of traditional Chinese medicine, can solve the problems of complex process, low purity and low ginkgolide yield, and achieves the effect of high extraction yield

Active Publication Date: 2004-04-28
CHENGDU BAIYU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the unique pharmacological effects of ginkgolides, and these ingredients are only found in one plant, Ginkgo biloba, due to the complex structure of this ingredient, it is currently impossible to produce it by organic synthesis.
[0004] At present, there are many reports on the extraction of ginkgolides, but the process is generally complicated, the yield of ginkgolides is not high, and the purity is not high. Only ginkgolides A and B can be extracted, but ginkgolide C cannot be extracted, which affects the medicinal value. , reducing the curative effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0046] Ginkgo biloba as raw material

[0047] Take 20 kg of ginkgo leaves, add 200 kg of 60% ethanol, heat and extract for 3 hours, filter, add 160 kg of 60% ethanol to the residue, heat and extract for 3 hours, filter, combine the extracts, concentrate under reduced pressure to 1 / 3 volume, and statically Leave it for 8 hours, centrifuge, put the supernatant on a polyamide column, collect the effluent, elute the polyamide column with 2%-5% ethanol, combine the eluate and effluent, put it on a macroporous adsorption resin column, and first use water Elution, then elution with 60% ethanol, steaming under reduced pressure to a small volume of about 20,000 ml, standing still, 70 grams of coarse crystals were precipitated, and the coarse crystals were recrystallized with 10 times the amount of methanol-water (1:1), and the solution Evaporate to a small volume, and precipitate total lactone crystals: 50g, containing A, B, and C.

example 2

[0049] Ginkgo biloba extract GBE as raw material

[0050] Take 500g of GBE (containing more than 6% ginkgolide), dissolve it with 50,000 ml of 2-5% ethanol, put it on a polyamide column for adsorption, collect the effluent, and elute the polyamide column with 100,000 ml of 2%-5% ethanol. The effluents were combined, concentrated under reduced pressure to a small volume of about 8,000 ml, and coarse crystals were precipitated after cooling.

[0051] The crude crystals were recrystallized with 10 times of methanol-water (1:1), and the solution was evaporated to a small volume to precipitate 16 g of total lactones, which combined A, B, and C.

[0052] The above-mentioned total lactone contents are all greater than 70%.

example 3

[0054] Ginkgolide preparation (dropping pill) formula is:

[0055] Ginkgolide 5~25g

[0056] PEG400 4~10g

[0057] PEG6000 10~20g

[0058] The amount of ethanol is sufficient to completely dissolve the ginkgolides

[0059] The above raw materials are made into 1000 drop pills.

[0060] Preparation method: Take ginkgolide and add a certain amount of ethanol to dissolve it, then add the prescribed amount of PEG400, PEG6000, heat and melt in a water bath, stir to mix completely, put it in the storage tank of the dropping pill machine, keep warm at 70-90°C, 30 At a speed of ~60 rpm, drop in methyl silicone oil cooled to 5~10°C, take out the dropping pills, absorb the coolant, dry, and obtain.

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Abstract

The extracting process of bilobalide A, B and C includes the polyamide column adsorption of the gingko extract as material, concentration and crystallization to obtain coarse crystal; or twice extraction of gingko leaf as material, concentration, filtering, polyamide column adsorption, collecting effluent, eluting polyamide column with alcohol, merging the effluent and the eluent, elution in macroporous resin column with alcohol, concentration and crystallization to obtain coarse crystal; and re-crystallizing the coarse crystal in methanol water to obtain bilobalide A, B and C. Bilobalide A, B and C may be produced into dripping pill, granule or capsule. The present invention has simple process, high yield, and product with bilobalide A, B and C content up to 70 %.

Description

technical field [0001] The invention relates to a method for extracting effective parts of traditional Chinese medicines, in particular to a process for extracting ginkgolides from ginkgo leaves or ginkgo leaf extracts. Background technique [0002] Ginkgolides have unique physiological effects and therapeutic value. Ginkgolides are strong platelet activating factor (PAF) antagonists, which mainly benefit the heart and astringe the lungs in clinical practice. They are used to treat cardiovascular and cerebrovascular diseases and cough. big. [0003] Platelet activating factor is a mammalian endogenous physiologically active substance, which is mainly related to allergies, ulcers, asthma, thrombosis, certain inflammations, allogeneic rejection of organ transplantation, myocardial damage caused by hypoxia in coronary heart disease patients, etc. The pathogenesis is closely related, therefore, platelet activating factor antagonists may be used in the prevention and treatment o...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/365A61P9/00A61P11/14C07D493/22
Inventor 杜安全周正华
Owner CHENGDU BAIYU PHARMA CO LTD
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