Bilobalide B raw material and preparation thereof

A ginkgolide and raw material technology, applied in the field of ginkgolide B raw material and its preparation, can solve the problems of less than 2%, low transfer rate, difficult to form industrialization, etc., and achieve cost saving, simple process and low cost Effect

Active Publication Date: 2008-11-12
YANGTZE RIVER PHARMA GRP JIA NGSU LONGFENGTANG TRADITIONAL CHINESE MEDICINE CO LTD +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The content of Ginkgolide B in Ginkgo biloba and Ginkgo leaf extract is very low. The ginkgo preparations that appear on the market currently mainly use total ginkgo lactones and total flavonoids as the effective parts, and there is no monomer Ginkgo preparation. Currently, Ginkgo The acquisition of ester B monomer is mainly prepared by liquid phase, and the transfer rate is very low, it is difficult to form industrialization
[0004] The published patent CN101054384A process through literature review requires two column chromatography, and the final transfer rate is less than 2%. The efficiency and final yield of the whole process are low, resulting in relatively high cost of ginkgolide B per unit weight

Method used

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  • Bilobalide B raw material and preparation thereof
  • Bilobalide B raw material and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Weigh 10 kg of ginkgo leaves, add 500L of 1% hydrochloric acid and soak for 30 minutes, filter to obtain 480L of soaking liquid, extract with 2400L of n-butanol, concentrate the extract to an appropriate amount, add an appropriate amount of 100-200 mesh silica gel, mix and dry, Go up silica gel column (diameter-to-height ratio is 1: 1, silica gel consumption 3kg), with ethyl acetate: acetone is the ratio preparation mobile phase of 4: 6, control flow rate 180ml / min, collect the 40L effluent containing ginkgolide B, Concentrate and dry to obtain 6g of dry cream, add 180ml of 95% ethanol to crystallize, and obtain 2.3g of ginkgolide B raw material, wherein, the content of ginkgolide B is 91.5%.

Embodiment 2

[0034] Weigh 20kg of ginkgo leaves, add 700L of 0.5% hydrochloric acid and soak for 150min, filter to obtain 650L of filtrate, extract with 1300L of acetone, concentrate the extract to an appropriate amount, add an appropriate amount of 100-200 mesh silica gel, mix and dry, and put on a silica gel column (diameter-to-height ratio is 1: 1, silica gel consumption 5.7kg), with ethyl acetate: sherwood oil is the ratio preparation mobile phase of 7: 3, control flow rate 410ml / min, collect 70L effluent, concentrate and dry to obtain 10g dry paste, Add 300ml of 95% ethanol to crystallize to obtain 4.1g of ginkgolide B raw material, wherein the content of ginkgolide B is 92.0%.

Embodiment 3

[0036] Weigh 1kg of Ginkgo biloba extract (in line with the requirements of "Chinese Pharmacopoeia" 2000 edition, Taiyuan Xingyuan Biochemical Co., Ltd.), add 5L of 0.1% hydrochloric acid and soak for 60min, filter to obtain 4.8L of filtrate, and extract with 9.6L of ethyl acetate , concentrate the extract to an appropriate amount, add an appropriate amount of 100-200 mesh silica gel, mix and dry, put on a silica gel column (the ratio of diameter to height is 1:1, and the amount of silica gel is 2.5kg), with n-butanol:petroleum ether as 8:2 Prepare the mobile phase according to the ratio, control the flow rate of 360ml / min, collect 35L of the effluent, concentrate and dry to obtain 5g of dry cream, add 150ml of 95% ethanol to crystallize, and obtain 1.7g of ginkgolide B raw material, wherein the content of ginkgolide B is 90.7% .

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Abstract

The invention discloses a ginkgolide B raw material, which is characterized in that: the ginkgolide B raw material is made through the following method that: ginkgo leaves or ginkgo leaf extracts are taken and boiled in a hydrochloric acid solution; the boiled liquid undergoes organic extraction after filtration; when the obtained extract is condensed, 100 to 200-mesh silica gel is added in the extract to be mixed and dried; silica gel column chromatography is used to collect eluent rich in ginkgolide B, and the ginkgolide B raw material is obtained through crystallization; and the content of ginkgolide B in the ginkgolide B raw material is more than or equal to 90 percent. The ginkgolide B raw material made through adopting the method has high purity of ginkgolide B, simple preparation technological process, high transfer rate and low cost, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and in particular relates to a ginkgolide B raw material and a preparation method thereof. technical background [0002] Ginkgolide is currently one of the most powerful and specific platelet activating factor (PAF) receptor blockers. Ginkgolide B has the strongest blocking effect on PAF receptor among ginkgolides, and can be eliminated in a dose-dependent manner. The platelet aggregation caused by PAF prevents the formation of thrombus, but has no effect on the platelet aggregation induced by adenosine diphosphate, arachidonic acid, collagen and epinephrine. The latest pharmacological studies show that ginkgolide B has anti-allergic, anti-inflammatory, anti-shock effects, and also has protective effects on ischemic injury and rejection of organ transplantation. [0003] The content of Ginkgolide B in Ginkgo biloba and Ginkgo leaf extract is very low. Currently, ginkgo prepar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61K36/16
Inventor 许益清徐林张朝波朱敬
Owner YANGTZE RIVER PHARMA GRP JIA NGSU LONGFENGTANG TRADITIONAL CHINESE MEDICINE CO LTD
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