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Baicalin ion pair medicine from traditional Chinese medicine of baikal skullcap root as well as preparation method and application thereof

A technology of baicalin ion and baicalin, which is applied to the field of baicalin ion pair medicine from traditional Chinese medicine Scutellaria baicalensis and its preparation and use, can solve the problems of difficult, unstable, water-soluble and fat-soluble baicalin and the like

Active Publication Date: 2010-09-08
曾建国
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, in long-term pharmaceutical research, the bioavailability of baicalin is limited because it is extremely poorly soluble in various inorganic and organic solvents, has poor water and fat solubility, and is unstable in lye.
In addition, long-term single use of traditional Chinese medicine components of baicalin will also lead to the emergence of drug-resistant strains, thus making its antibacterial spectrum not broad enough

Method used

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  • Baicalin ion pair medicine from traditional Chinese medicine of baikal skullcap root as well as preparation method and application thereof
  • Baicalin ion pair medicine from traditional Chinese medicine of baikal skullcap root as well as preparation method and application thereof
  • Baicalin ion pair medicine from traditional Chinese medicine of baikal skullcap root as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: the preparation method of baicalin ion pair compound

[0043] Dissolve 20.0 g of chelerythrine hydrochloride (provided by Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 1000 mL of water, heat to above 90°C until all chelerythrine hydrochloride is dissolved, and filter to make white Dronerythrine hydrochloride aqueous solution (A); 24.4 g of baicalin sodium salt (provided by Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) was dissolved in 200 mL of water and filtered to prepare baicalin sodium salt aqueous solution (B); above 90 ° C Slowly add baicalin sodium salt aqueous solution (B) to chelerythrine hydrochloride aqueous solution (A) under certain conditions, stir continuously, react for 2 hours, cool to room temperature, filter, wash the precipitate fully with pure water, the precipitate 60 °C and vacuum-dried to obtain 40.2 g of the baicalin ion-pair compound.

Embodiment 2

[0044] Embodiment 2: the preparation method of baicalin ion pair compound

[0045] Dissolve 20.0 g of chelerythrine bisulfate (provided by Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 1000 mL of water, heat to above 90°C until all chelerythrine bisulfate is dissolved, and adjust the pH to 7. Filter to make chelerythrine bisulfate aqueous solution (A); dissolve 21.0 g of baicalin sodium salt in 200 mL and filter to prepare baicalin sodium salt aqueous solution (B); make baicalin sodium salt aqueous solution (B) under conditions above 90°C Slowly add glycoside sodium salt solution (B) into chelerythrine bisulfate aqueous solution (A), stir continuously, react for 2 hours, cool to room temperature, filter, wash the precipitate fully with pure water, and vacuum dry the precipitate at 60°C. That is, 35.7 g of the ion pair compound of baicalin was obtained.

Embodiment 3

[0047] Preparation method of baicalin ion pair compound

[0048] Dissolve 20.0 g of chelerythrine hydrochloride in 1000 mL of water, heat to above 90° C. until all chelerythrine hydrochloride (provided by Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) is dissolved, and filter to make white Dronerythrine hydrochloride aqueous solution (A); 25.2 g of baicalin potassium salt was dissolved in 200 mL of water and filtered to prepare baicalin potassium salt solution (B); under conditions above 90 ° C, baicalin potassium salt solution (B) Slowly add to chelerythrine hydrochloride aqueous solution (A), stir continuously, react for 2 hours, cool to room temperature, filter, wash the precipitate with pure water, and dry the precipitate in vacuum at 60°C to obtain the baicalin ion pair compound 40.7g.

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Abstract

The invention relates to a novel baicalin ion pair compound which is an ion pair compound having the structure of a formula (I) and containing baicalin. The baicalin ion pair compound is an ion pair compound generated by the baicalin and chelerythrine. The spectrum analysis of 1H-NMR, 13C-NMR, MS, IR and UV proves that the molecular formula of the ion pair compound is C42H35015N. By the sieving of the antibacterial activity, the ion pair compound has the antibacterial activity, and the activity is obviously better than that of the baicalin. The invention also relates to a human medicine, a veterinary medicine or a daily health product of the baicalin ion pair compound in the antibacterial aspect.

Description

technical field [0001] The invention relates to a baicalin ion-pair drug from the traditional Chinese medicine Scutellaria baicalensis and a preparation method thereof, and the pharmaceutical use of the drug in antibacterial aspects, specifically human medicine, veterinary medicine and daily chemical products. 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 isolated clinically to certain drugs has ranked first in the world. For example, 80% of Staphylococcus aureus infected in Shanghai have developed resistance to penicillin G. The application of third-generation cephalosporin antibiotics such as Claforon and ceftriaxone has become more and more common...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/00C07D491/056A61K31/7048A61K31/4355A61P29/00A61K8/60A61K8/49A23K1/14
Inventor 曾建国谈满良贺晓华杜方麓
Owner 曾建国
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