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Ion-pair compounds of sanguinarine from Chinese herbs extract, and preparation and applications thereof

A technology of compounds and ion pairs, which is applied in the preparation of organic compounds, drug combinations, steroids, etc., can solve the problems of increasing the difficulty of sanguinarine compound drugs, increasing the difficulty of reaction, and increasing production costs, etc., to achieve long-term benefits Preservation and in vivo use, enhance drug efficacy, increase the effect of stability

Active Publication Date: 2010-07-21
曾建国
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in this method, two macromolecular groups with similar physical and chemical properties and the same pharmacological effects must be selected for compounding. After entering the body, the two molecules will dissociate and exert their medicinal effects. Alkali has similar physical and chemical properties and the same pharmacological effects as the compound of traditional Chinese medicine extract, which not only increases the production cost and increases the difficulty of the reaction, but also has to be based on the "jun, minister, adjuvant and envoy" drug division relationship of Chinese herbal medicine To determine the primary and secondary / proportional relationship of the two medicinal ingredients, and to rely on numerous clinical experiments to prove whether the two medicinal active ingredients can produce a synergistic effect, this undoubtedly increases the difficulty of developing sanguinarine compound drugs

Method used

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  • Ion-pair compounds of sanguinarine from Chinese herbs extract, and preparation and applications thereof
  • Ion-pair compounds of sanguinarine from Chinese herbs extract, and preparation and applications thereof
  • Ion-pair compounds of sanguinarine from Chinese herbs extract, and preparation and applications thereof

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Experimental program
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Effect test

Embodiment 1

[0047] Embodiment 1: The preparation method of the ion-pair compound generated by sanguinarine hydrochloride and sodium shikimate

[0048] Dissolve 10.0 g of sanguinarine hydrochloride (provided by Hunan Traditional Chinese Medicine Extraction Engineering Research Center) in 1000 mL of water, heat to above 90°C until all sanguinarine hydrochloride is dissolved, and make sanguinarine hydrochloride aqueous solution (A); 1.1 g of sodium shikimic acid salt was dissolved in 200 mL of water to prepare sodium shikimic acid salt aqueous solution (B);

[0049] Slowly add (B) to (A) at a temperature above 90°C, stir continuously at 90°C, react for 30 minutes, cool to room temperature, filter the precipitate, wash the precipitate fully with pure water, and dry the precipitate in vacuum at 60°C to obtain a light yellow color crystals, conduct 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is an ion pair compound of sanguinarine shikimic acid.

Embodiment 2

[0050] Example 2: The preparation method of the ion-pair compound generated by sanguinarine and carnosic acid

[0051] Dissolve 10.0 g of sanguinarine (provided by the Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 2000 mL of ethanol, and stir to dissolve. Then directly add carnosic acid 10.0g, stir at normal temperature for 45min, concentrate, dry to obtain precipitate, then refine with ethyl acetate to obtain light yellow crystal, by carrying out 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is the ion-pair compound of sanguinarine carnosic acid.

Embodiment 3

[0052] Embodiment 3: The preparation method of the ion-pair compound generated by sanguinarine hydrochloride and sodium rosmarinate

[0053] Dissolve 4.5 g of sanguinarine hydrochloride (provided by the Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 1 L of water, then add 4.0 g of sodium rosmarinate, stir at 80 ° C for 30 min, after cooling, filter the precipitate, wash, and dry , and further refined with methanol to obtain pale yellow crystals. by carrying out 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is an ion pair compound of sanguinarine sodium rosmarinate.

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Abstract

The invention relates to a preparation method and applications of ion-pair compounds of sanguinarine. In the invention, sanguinarine reacts with an organic acid, and the organic acid mainly comprises chlorogenic acid, gallic acid, shikimic acid, oleanolic acid, ursolic acid, benzoic acid, salicylic acid, tartaric acid, lactic acid, sorbic acid, fumaric acid, malic acid, citric acid, maleic acid, glycyrrhizic acid, glycyrrhetinic acid, carnosic acid, hydroxyci amic acid, rosmarinic acid, succinic acid, ferulic acid, protocatechuic acid, cinnamic acid, caffeic acid, chicoric acid or pseudolaricacid B. The ion-pair compounds prepared from sanguinarine and organic acids have the bioactivity of antibiosis. The invention also relates to applications of ion-pair compounds containing sanguinarine in medicaments, veterinary medicines or daily chemicals.

Description

technical field [0001] The present invention relates to an ion-pair drug and preparation method of sanguinarine from a traditional Chinese medicine extract, and the pharmaceutical use of the drug in antibacterial aspects, especially in human medicine, veterinary medicine and daily chemical products, especially involving sanguinarine containing sanguinarine The ion pair compound formed by alkali and organic acid is used in the preparation of veterinary medicine or daily chemical products, especially the application of veterinary medicine and drug feed additive in the direction of animal antibacterial. Background technique [0002] In recent years, due to the abuse of antibiotics by humans, the resistance of bacteria to various antibiotics has been showing a rapid upward trend. China is one of the countries with the most serious abuse of antibiotics in the world, and the resulting problem of bacterial resistance is particularly prominent. The resistance of some bacteria isola...

Claims

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Application Information

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IPC IPC(8): C07D491/153A61K31/4741C07C69/732C07C67/28C07C65/03C07C51/41A61K31/192A61K31/216A61K31/19C07C62/32C07J63/00C07C62/06C07C63/08C07C65/10A61K31/60A61P29/00A61P31/04A61P31/10A61P31/12A23K1/17A23K20/195
Inventor 曾建国谈满良贺晓华杜方麓
Owner 曾建国
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