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Novel application of catechin compounds in preparation of medicaments for treating hyperuricemia

A technology of hyperuricemia and catechin gallate, applied in the field of chemical medicine, can solve the problems of irritation, large toxic and side effects of drugs, triggering acute gout attacks, etc., and achieves high safety, no toxic side effects, and lower serum uric acid. horizontal effect

Inactive Publication Date: 2015-11-11
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 severe toxic side effects such as allergic reaction (morbidity rate 10-15%), hypersensitivity syndrome, myelosuppression; Probenecid, benzbromarone can stimulate gastrointestinal tract, cause kidney Side effects such as colic and acute gout attacks limit the clinical application of these drugs to a certain extent

Method used

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  • Novel application of catechin compounds in preparation of medicaments for treating hyperuricemia
  • Novel application of catechin compounds in preparation of medicaments for treating hyperuricemia
  • Novel application of catechin compounds in preparation of medicaments for treating hyperuricemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Preparation and Characterization of Example 1 Gallocatechin GC

[0025] 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:

[0026] GCC 15 h 14 o...

Embodiment 2

[0029] Example 2 Preparation and Characterization of Catechin Gallate CG

[0030] 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:

[0031] CGC ...

Embodiment 3

[0034] Example 3 Preparation and Characterization of Gallocatechin Gallate GCG

[0035] 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 data ...

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Abstract

The invention discloses gallocatechin, catechin gallate or gallocatechin gallate and application of its pharmaceutically acceptable salts in treating hyperuricemia. The catechin compounds has high in-vitro inhibitory action on xanthine oxidase, also can evidently decrease serum uric acid levels in mice with hyperuricemia, and can serve as a potential xanthine oxidase inhibitor and a potential uric-acid-lowering medicament to treat 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, which 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 n...

Claims

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Application Information

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