Diphenyl ethylene glycosides derivatives

A technology of stilbene glycosides and ethanol, which is applied in the field of medicine, can solve the problems that the purity of stilbene glycosides is far from meeting the quality requirements, cannot meet industrial production, and the process is cumbersome, etc., and achieves the improvement of large dosage, less impurities, and drug efficacy. exact effect

Inactive Publication Date: 2008-09-03
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

These documents are also based on basic research carried out in laboratory research, and the amount of resin used is generally only a few grams, which is still incomparable with industrial production processes, and the purity of the stilbene glycosides obtained is far from that of monomers. Quality requirements
[0008] In addition, Chinese patent ZL 98120290.X discloses a met

Method used

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  • Diphenyl ethylene glycosides derivatives
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  • Diphenyl ethylene glycosides derivatives

Examples

Experimental program
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Example Embodiment

[0048] Example 1

[0049] Take 100kg of dried Polygonum multiflorum medicinal materials, cut them into 1-3mm slices, put them into a hot reflux extraction tank, add 10 times the amount of water and an appropriate amount of sodium sulfite, adjust the pH of the extract to 7.6, and extract by heating and refluxing for 3 times, 1 hour each time, The extracts were combined, filtered, and the filtrate was collected. The filtrate was passed through a HPD-400 macroporous adsorption resin column, eluted with 500 L of water, and eluted with 80% ethanol to collect the eluate containing stilbene glycosides, a total of 200 L, concentrated under reduced pressure at 60 °C to 10 L, and added ethyl acetate. Ester extraction was performed three times, each using 10 L, and the ethyl acetate solution was concentrated to dryness under reduced pressure at 60° C. to obtain 2.5 kg of crude stilbene glycoside extract.

[0050] Take the above crude extract, add 5.0L of ethanol, heat and stir to fully ...

Example Embodiment

[0052] Example 2

[0053] Take 100kg of dried Polygonum multiflorum medicinal materials, pulverize it into coarse powder, put it into a hot reflux extraction tank, add 8 times the amount of water and an appropriate amount of sodium bisulfite, adjust the pH of the extraction solution to 7.5, and extract by heating and refluxing twice, 2 hours each time, The extracts were combined, filtered, and the filtrate was collected. The filtrate was passed through an HPD-100 macroporous adsorption resin column, eluted with 600 L of water, and then eluted with 70% ethanol. The eluate containing stilbene glycosides was collected, totaling 300 L, concentrated under reduced pressure at 70 °C to 15 L, and n-butyl was added. Alcohol extraction was performed twice, each time using 15 L, concentrated under reduced pressure at 80°C, and concentrated n-butanol to dryness to obtain 2.3 kg of stilbene glycoside crude extract.

[0054] Take the above crude extract, add 8.0 L of ethyl acetate, heat an...

Example Embodiment

[0056] Example 3

[0057] Take 120kg of dried Polygonum multiflorum, pulverize it into coarse powder, put it into a hot reflux extraction tank, add 7 times the amount of water and an appropriate amount of sodium carbonate, adjust the pH of the extraction solution to 7.8, heat and reflux for 3 times, 1.5 hours each time, combine and extract liquid, filter, and collect the filtrate. The filtrate was passed through an AB-8 macroporous adsorption resin column, 600 L of water was added to elute, and then 90% ethanol was added to elute to collect the eluate containing stilbene glycosides, a total of 320 L, concentrated under reduced pressure at 70 °C to 20 L, and ethyl acetate was added. Ester extraction was carried out 3 times, each using 20 L, concentrated under reduced pressure at 80°C, and concentrated ethyl acetate to dryness to obtain 2.92 kg of stilbene glycoside crude extract.

[0058] Take the above crude extract, add 12L of acetone, heat and stir to fully dissolve it, fil...

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Abstract

The invention relates to a new type 2, 3, 5, 4'- tetra-hydroxyl diphenyl ethylene-2-O-beta-D-glucoside crystal, a method for making same, and pharmaceutical compositions containing the crystal. The content of the crystal is 90-99. 9tested by high performance liquid chromatography, and the stilbene glucoside crystal of high-purity is obtained by abstracting fleece-flower root, extracting with an organic solvent, separating by column chromatography and crystallizing in appropriate dissolvent. The preparing process provides high yield, low cost, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a separation and purification process of effective monomer 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in Radix Polygoni Multiflori; also relates to 2,3,5 , Crystal of 4'-tetrahydroxystilbene-2-O-β-D-glucoside, preparation method thereof, and pharmaceutical composition containing it as main component. Background technique [0002] Polygonum multiflorum is the tuber root of Polygonum multiflorum Thunb., which is a commonly used traditional Chinese medicine with a long history of medicinal use. A large number of research results at home and abroad show that Polygonum multiflorum has many functions such as immune regulation, liver protection, anti-oxidation, anti-tumor, and blood fat reduction. pharmacological activity. With the deepening of research, the research on its chemical composition has become more and more clear. A large number of studies have shown that the main role ...

Claims

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Application Information

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IPC IPC(8): C07H15/203A61K31/7034A61K36/704A61P39/06A61K125/00
Inventor 杨永安王鸯
Owner NANJING CHIA TAI TIANQING PHARMA
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