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Medicinal composition for treating gout

A composition and drug technology, applied in the field of pharmaceutical preparations, can solve the problems of liver function damage, aggravation of gout attacks and the like

Inactive Publication Date: 2010-12-29
TIANJIN TAIPU PHARMA SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are also literatures showing that taking large doses of febuxostat can significantly damage liver function.
[0004] (2) Drugs that promote uricosuric agents, such as probenecid, sulfinpyrazone, etc., but they all have different degrees of side effects and toxicity, especially probenecid, which can cause gout pain in the early stage of treatment. Aggravated attacks, possibly due to movement of urate from the joint

Method used

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  • Medicinal composition for treating gout
  • Medicinal composition for treating gout
  • Medicinal composition for treating gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation of febuxostat crystals:

[0054] Take 2 grams of febuxostat, dissolve it in 60ml of 95% ethanol, cool down, let it stand naturally, precipitate crystals, filter, and dry to obtain 1.94 grams of febuxostat crystals, with a yield of 85%, and then perform SXRD determination. Results: The febuxostat crystal is monoclinic, its space group is P2(1), and the unit cell parameters are: a=4.7179(9) b=17.813(4) c=10.690(2) α=γ=90°, β=99.20(3)°, the unit cell volume is: 886.8(3) For details, please refer to the preparation method disclosed in the application number: 200910068558.2.

Embodiment 2

[0056] Probenecid 1000g, febuxostat crystal 11.5g (equivalent to febuxostat 10g), lactose 675g, microcrystalline cellulose 250g, mix well, add appropriate amount of 10% PVP-ethanol solution to granulate, dry, then add Carboxymethyl starch sodium 83g, magnesium stearate 23.5g, mix well, tablet, film-coated.

Embodiment 3

[0058] Preparation of tablets: mix probenecid 750g, febuxostat crystal 22.9g (equivalent to febuxostat 20g), add lactose 1667g, pregelatinized starch 390g, hydroxypropyl cellulose 15g, cross-linked carboxylate Sodium methylcellulose 63g, magnesium stearate 31.5g, mixed evenly, granulated with pure water, dried, compressed into tablets, coated with film.

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Abstract

The invention relates to a medicinal composition for treating gout. The composition consists of febuxostat crystals, probenecid and a pharmaceutically acceptable medicinal carrier of which the ratio of part by weight is 1:10-200:0.05-100. When the ratio of the febuxostat crystals to the probenecid is 1 to 33.3, the inhibition ratio is improved by 155.6 percent compared with the total inhibition rate of the febuxostat crystals and the probenecid which are singly used; and when the ratio of the febuxostat crystals to the probenecid is 1 to 100, the inhibition ratio is improved by 113.3 percent compared with the total inhibition ratio of the febuxostat crystals and the probenecid which are singly used. Pharmacological tests show that the composition has obvious synergetic effect, can quickly reduce the concentration of uric acid in blood serum, obviously improves gout treatment effect, greatly reduces the dosage of each single component at the same time and effectively reduces the toxic and side effects of the medicament.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition composed of febuxostat crystals and probenecid, and the application of the composition in the treatment of acute and chronic gout. Background technique [0002] Gout is a group of inherited or acquired disorders of uric acid metabolism. The cause of gout is abnormal uric acid metabolism, resulting in high blood uric acid. Uric acid is the final product of the catabolism of purine compounds in the human body. Increased uric acid production or decreased renal uric acid excretion can lead to increased blood uric acid. Therefore, there are currently two main categories of drugs for the treatment of gout: [0003] (1) Drugs that reduce the production of uric acid, such as allopurinol, febuxostat, etc., which reduce the production of uric acid by inhibiting the activity of xanthine oxidase, thereby reducing the uric acid content in blood...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K31/192A61P19/06A61P19/02A61P13/12
Inventor 张殿镇赵健朱红星
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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