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New application of catechin compound and gallic acid combination to preparation of hyperuricemia treatment medicine

A technology of hyperuricemia and catechins, applied in the field of pharmaceutical compositions that can treat hyperuricemia and gout, can solve the problems of stimulating acute attacks of gout, large toxic and side effects of drugs, and weak inhibitory effect. Toxic and side effects, lower serum uric acid level, strong in vitro inhibitory effect

Active Publication Date: 2015-10-21
江苏凯吉生物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Both of the above methods can reduce uric acid in the blood, and then produce curative effects on diseases such as gout, arthritis, subcutaneous gout stones, kidney stones or gouty nephropathy caused by hyperuricemia, but the side effects of the above drugs are usually relatively high. Large, for example, allopurinol can cause allergic reactions (incidence rate 10‐15%), hypersensitivity syndrome, bone marrow suppression and other serious side effects; probenecid and benzbromarone can stimulate the gastrointestinal tract, cause renal Side effects such as colic and acute gout attacks limit the clinical application of these drugs to a certain extent
[0006] Catechin is a compound widely present in plants, literature ["Inhibition of Xanthine Oxidase by Flavonoids", 1999,63(10), 1787‐17904381‐4385], ["Inhibition of Xanthine Oxidase by Catechins from Tea( Camellia sinensis)", 1997, vol.17, p.4381‐4385] have reported the xanthine oxidase inhibitory effect of C, EC, EGC, ECG, EGCG these catechins and epicatechin, and research The results showed that among the five catechins and epicatechins, EGCG had better activity, while the other four compounds had weaker inhibitory effects.

Method used

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  • New application of catechin compound and gallic acid combination to preparation of hyperuricemia treatment medicine
  • New application of catechin compound and gallic acid combination to preparation of hyperuricemia treatment medicine
  • New application of catechin compound and gallic acid combination to preparation of hyperuricemia treatment medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation and Characterization of Example 1 Gallocatechin GC

[0026] Get 10g epigallocatechin (EGC) and dissolve in 1000mL McIlvaine buffer solution (pH5.0), be placed in autoclave, 120 ℃ of reaction 30 minutes, take a sample after reaction finishes, high performance liquid chromatography analysis result shows that conversion rate 62%; after the reaction solution was concentrated, it was separated and purified by preparative HPLC (C18 chromatographic column 5U, 50*500mm), eluted with a gradient of 10%-95% ethanol, and the GC components with a purity higher than 94% were collected and concentrated Remove part of the ethanol, add 3 times the amount of water and continue to concentrate. When the solution becomes turbid, stop the concentration and place it for overnight crystallization, filter, and freeze-dry the crystals to obtain monomer compound gallocatechin (GC) with a purity of 99.3%. The detection and characterization data are as follows:

[0027] GC C 15 h 14 ...

Embodiment 2

[0030] Example 2 Preparation and Characterization of Catechin Gallate CG

[0031] Get 10g epicatechin gallate (ECG) and dissolve in 1000mL McIlvaine buffer solution (pH5.0), be placed in autoclave, 120 ℃ of reaction 30 minutes, take a sample after reaction finishes, high performance liquid chromatography analysis result shows, The conversion rate was 56%; after the reaction solution was concentrated, it was separated and purified by preparative HPLC (C18 chromatographic column 5U, 50*500mm), eluted with a gradient of 20%-95% ethanol, and the CG component with a purity higher than 94% was collected , Concentrate to remove part of the ethanol, add 3 times the amount of water and continue to concentrate, when the solution becomes turbid, stop concentrating and place it overnight for crystallization, filter, freeze-dry the crystals to obtain the monomeric compound catechin gallate with a purity of 98.9% (CG). The detection and characterization data are as follows:

[0032] CG C ...

Embodiment 3

[0035] Example 3 Preparation and Characterization of Gallocatechin Gallate GCG

[0036] Get 10g epigallocatechin gallate (EGCG) and dissolve in 1000mL McIlvaine buffer solution (pH5.0), be placed in autoclave, 120 ℃ of reaction 30 minutes, take a sample after reaction finishes, high-performance liquid chromatography analysis result shows , the conversion rate was 56.5%; after the reaction solution was concentrated, it was separated and purified by preparative HPLC (C18 chromatographic column 5U, 50*500mm), eluted with a gradient of 15%-95% ethanol, and the GCG group with a purity higher than 94% was collected Divide, concentrate to remove part of ethanol, add 3 times the amount of water and continue to concentrate, when the solution becomes turbid, stop the concentration and place it overnight for crystallization, filter, freeze-dry the crystals to obtain the monomer compound gallocatechin gallate with a purity of 99.1% acid ester (GCG). The detection and characterization dat...

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Abstract

The invention discloses combined application of gallnut catechin or catechin gallate or gallnut catechin gallate and salt capable of being pharmaceutically accepted and gallic acid to treating hyperuricemia. A catechin compound has the strong in-vitro inhibition effect on xanthine oxidase, the serum uric acid level of a mouse suffering from hyperuricemia can be obviously reduced, and the catechin compound can serve as a potential xanthine oxidase inhibitor and a uric acid reduction medicine to be used for treating hyperuricemia and gout or gout complications caused by hyperuricemia.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and in particular relates to the application of a catechin compound and a pharmaceutically acceptable salt thereof in the preparation of a drug for treating hyperuricemia, and a drug combination capable of treating hyperuricemia and gout thing. Background technique [0002] In recent years, with the improvement of people's living standards and changes in dietary structure, the intake of sugar, fat, and protein has increased significantly, and the incidence of hyperuricemia and gout has increased day by day, and has become a common disease. [0003] It is generally believed that when the blood uric acid is 416 μmol / L, it is hyperuricemia, and about 5%‐12% of patients with hyperuricemia will develop gout. The clinical features are: recurrent gouty acute arthritis, tophi deposition, characteristic chronic arthritis and joint deformities, often involving the kidneys to cause chronic interstitial nep...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61P19/06A61P19/02A61P13/12A61P13/04A61P9/00A61K31/192
Inventor 温尧林张小芸
Owner 江苏凯吉生物科技有限公司
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