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Chlorogenic acid compound and pharmaceutical composition thereof

A chlorogenic acid and compound technology, applied in the field of medicine, can solve problems such as poor stability of chlorogenic acid, and achieve the effects of improving drug safety, high bioavailability and stable quality

Active Publication Date: 2012-10-24
ZHEJIANG WECOME MEDICINE IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the above-mentioned patents and prior art, although the content of the active ingredient chlorogenic acid has been increased and a large amount of impurities have been removed, the problem of poor stability of chlorogenic acid has not been solved. In view of this, the present invention is proposed

Method used

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  • Chlorogenic acid compound and pharmaceutical composition thereof
  • Chlorogenic acid compound and pharmaceutical composition thereof
  • Chlorogenic acid compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation of Chlorogenic Acid Compound Crystals

[0044] Dissolve the crude chlorogenic acid in the mixed solution of acetone / isobutanol, wherein acetone and isobutanol are formulated into a mixed solution at a volume ratio of 2:1, and the volume dosage of the mixed solution of acetone / isobutanol is the weight of the crude chlorogenic acid Adjust the pH to 3 with glacial acetic acid, then add activated carbon, stir for adsorption, filter for decarbonization and sterilization, heat to 55°C and stir at constant temperature for 2 hours, then cool down at a rate of 0.7°C / min and under stirring conditions Slowly add ether for crystallization, lower the temperature to 0°C, the stirring rate of adding ether for crystallization is preferably 12rmp, the amount of ether used is 3 times the volume of the acetone / isobutanol mixed solution, filter, dry under reduced pressure, and wash to obtain chlorogenic acid crystals.

[0045] The particle size of the chlorogenic acid crystals...

Embodiment 2

[0048] Preparation of Chlorogenic Acid Compound Crystals

[0049] Dissolve the crude chlorogenic acid in the mixed solution of acetone / isobutanol, wherein acetone and isobutanol are formulated into a mixed solution at a volume ratio of 3:1, and the volume dosage of the mixed solution of acetone / isobutanol is the weight of the crude chlorogenic acid Adjust the pH to 4 with glacial acetic acid, then add activated carbon, stir for adsorption, decarburize and sterilize by filtration, heat to 65°C and stir at constant temperature for 3 hours, then cool down at a rate of 1.2°C / min and under stirring conditions Slowly add diethyl ether for crystallization, lower the temperature to 5°C, the stirring speed of adding diethyl ether for crystallization is preferably 16rmp, the amount of diethyl ether is 4 times the volume of the acetone / isobutanol mixed solution, filter, dry under reduced pressure, and wash to obtain chlorogenic acid crystals.

[0050] The particle size of the chlorogeni...

Embodiment 3

[0053] Preparation of Chlorogenic Acid Compound Crystals

[0054] Dissolve the crude chlorogenic acid in the mixed solution of acetone / isobutanol, wherein acetone and isobutanol are formulated into a mixed solution at a volume ratio of 3:1, and the volume dosage of the mixed solution of acetone / isobutanol is the weight of the crude chlorogenic acid Adjust the pH to 4 with glacial acetic acid, then add activated carbon, stir for adsorption, decarburize and sterilize by filtration, heat to 60°C and stir at constant temperature for 2 hours, then cool down at a rate of 0.9°C / min and keep stirring Slowly add ether for crystallization, lower the temperature to 3°C, the stirring speed of adding ether for crystallization is preferably 15rmp, the amount of ether used is 4 times the volume of the acetone / isobutanol mixed solution, filter, dry under reduced pressure, and wash to obtain chlorogenic acid crystals.

[0055] The particle size of the chlorogenic acid crystals is 75-250 μm, t...

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a chlorogenic acid compound. The chlorogenic acid compound is crystal, which has the characteristic peaks in X-ray powder distraction pattern measured through Cu-K alpha ray at 2 theta of 7.9 degrees, 8.4 degrees, 8.8 degrees, 10.2 degrees, 12.0 degrees, 15.4 degrees, 16.9 degrees, 19.0 degrees, 21.9 degrees, 22.6 degrees, 25.9 degrees, 28.0 degrees, 29.6 degrees, and 35.1 degrees+ / -0.2 degree. The invention further relates to a pharmaceutical composition which comprises honeysuckle extract and radix scutellariae extract, wherein the radix scutellariae extract contains the chlorogenic acid compound crystal. Peripherally, the pharmaceutical composition is honeysuckle and radix scutellariae dispersible tablet and honeysuckle and radix scutellariae dripping pill. The chlorogenic acid compound and the pharmaceutical composition thereof provided by the invention have good stability, and the contents of related substances are less for long-term storage, so the pharmaceutical safety of a patient is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a chlorogenic acid compound and a pharmaceutical composition thereof. Background technique [0002] Chlorogenic acid, Chinese alias: (1S,3R,4R,5R)-3-[[3-(3,4-dihydroxyphenyl)-1-oxo-2-propenyl]oxy]-1,4 ,5-Trihydroxycyclohexanecarboxylic acid, English name: Chlorogenic acid, molecular formula is C 16 h 18 o 9 , the molecular weight is 354.31. Chlorogenic acid is an important biologically active substance, which has a wide range of antibacterial effects, is beneficial to gallbladder, hemostasis, increases white blood cells and antiviral effects, and has the effect of shortening blood coagulation and bleeding time. It is used to treat upper respiratory tract infection, anti-inflammatory and antipyretic , cooling blood to dissipate heat. Chlorogenic acid is an ester formed by caffeic acid and quinic acid. Its molecular structure has three unstable parts: ester bond, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/732A61K36/539A61K36/355A61K36/533A61K31/216A61P29/00A61P31/00A61P31/12A61P7/04
Inventor 刘忠良阮鸿献
Owner ZHEJIANG WECOME MEDICINE IND
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