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Active component having synergistic effect together with hyperuricemia treatment medicine, and febuxostat composition of active component

A technology of hyperuricemia and active ingredients, applied in the field of chemical medicine, can solve problems such as adverse reactions, achieve high safety, suppress adverse reactions, and reduce toxic and side effects

Active Publication Date: 2016-12-07
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The second technical problem to be solved by the present invention is the problem that febuxostat in the prior art can cause many adverse reactions, and then provide a method that can reduce the effect of febuxostat while maintaining the ideal uric acid-lowering effect. Febuxostat composition with toxic side effects

Method used

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  • Active component having synergistic effect together with hyperuricemia treatment medicine, and febuxostat composition of active component
  • Active component having synergistic effect together with hyperuricemia treatment medicine, and febuxostat composition of active component
  • Active component having synergistic effect together with hyperuricemia treatment medicine, and febuxostat composition of active component

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Extraction and characterization of compound 1-3 of the present invention

[0039] Take 5 kg of emblica medicinal material, pulverize it, and extract it with 5 L of water for 40 min while keeping it slightly boiling. The extract was concentrated to 1 L in vacuo, and the concentrated solution was separated by column chromatography using Diaion HP-20 macroporous adsorption resin, and eluted with water, 30% ethanol, 60% ethanol, and 95% ethanol respectively. Take 20 g of the eluent eluted with water and use reverse phase C18 silica gel for column chromatography separation, and use 5%-10% ethanol as the eluent for elution to obtain compound 1, compound 2 and compound 3 of the present invention respectively ;

[0040] The structural formula of the compound 1 is as follows:

[0041]

[0042] The structural formula of the compound 2 is as follows:

[0043]

[0044] The structural formula of the compound 3 is as follows:

[0045]

[0046] The detection and ...

Embodiment 2

[0053] Embodiment 2: Preparation and characterization of compound 4 of the present invention

[0054] In this example, Compound 4 of the present invention was prepared using the following synthetic route:

[0055]

[0056] The specific operation is as follows:

[0057] (1) Synthesis of 3,4,5-tribenzylbenzoic acid

[0058] Dissolve 17.0 g of gallic acid in 800 ml of dimethylformamide (abbreviated as DMF, the same below), and use nitrogen protection, add 113 g of anhydrous potassium carbonate in batches at 25 ° C, stir for 1 hour, heat up to 40 ° C, and then Add 143ml of benzyl bromide dropwise to the reaction system within 30min; after the dropwise addition, stir the reaction mixture at 40°C for 12h; use TLC to confirm that the reaction is complete, stop heating, and lower the reaction temperature to Room temperature 25°C; add 400ml of water and 1L of ethyl acetate to the reaction system, separate liquid extraction, wash the organic phase with 500ml of water three times, t...

Embodiment 3

[0069] Embodiment 3: Preparation and characterization of compound 5 of the present invention

[0070] In this example, compound 5 of the present invention was prepared using the same synthetic route and method as compound 4, the only difference being that the n-butanol in step 3) was replaced with 3-hydroxymethyl-benzoic acid to obtain this compound Invention compound 5, its structural formula is as follows:

[0071]

[0072] The detection and characterization data of the product are as follows:

[0073] Compound 5: C 15 h 12 o 7 , molecular weight 305[M+H] +

[0074] 1 H NMR (400MHz, CD 3 OD)δ8.14(s,1H),8.05(s,1H),7.81(d,1H),7.45(t,1H),6.95(s,2H),5.26(s,2H); 13 C NMR (100MHz, CD 3 OD) δ169.3, 165.9, 146.1.146.1, 141.1, 140.3, 132.3, 130.4, 129.2, 128.8, 128.6, 121.2, 109.6, 109.6, 65.7. It can be seen that its structure is correct.

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Abstract

The invention discloses an active component having a synergistic effect together with a hyperuricemia treatment medicine. The active component is plant polyphenol with the structure represented by formula (I) and a pharmaceutically acceptable salt of the plant polyphenol. The invention also provides a febuxostat composition. The febuxostat composition comprises febuxostat and the active component having a synergistic effect together with the hyperuricemia treatment medicine. The active component having a synergistic effect together with the hyperuricemia treatment medicine, and acts together with the hyperuricemia treatment medicine in the prior art in order to reduce the toxic and side effects of the hyperuricemia treatment medicine and keep an ideal uric acid reduction effect, and the active component has a synergistic medicine effect in the treatment process of hyperuricemia and hyperuricemia induced gouts or gout complications.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to an active ingredient having a synergistic effect with a drug for hyperuricemia, an application, a febuxostat composition and an application thereof. Background technique [0002] In the field of chemical medicine, uric acid is the terminal metabolite of human purine compounds. Disorders of purine metabolism lead to hyperuricemia. Under a normal purine diet, if the blood uric acid level is higher than 416 μmol / L in men and higher than 360 μmol / L in women twice on different days, it is called hyperuricemia. Usually, there is no subjective symptom in the pure state of hyperuricemia, but if the state is left alone for a long time, the urate in the blood will crystallize, and the crystallized urate will be deposited in the joints, subcutaneous tissue, kidneys, etc. Then there is a series of clinical manifestations such as gout and gout complications. With the change of p...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61K31/235A61K31/365A61K31/166A61K31/198A61K31/192A61K31/426A61P19/06A61P19/02A61P13/12A23L1/30C07C69/84C07H13/08C07D307/33C07C235/46C07C235/52C07C65/03
Inventor 温尧林
Owner CATCH BIO SCI & TECH
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