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Febuxostat and drug combination thereof

A technology for febuxostat and a composition, which is applied in the field of drug synthesis and can solve the problems of undisclosed compound crystal data, undisclosed data of ethanol solvation crystal structure determination of febuxostat, and the like

Inactive Publication Date: 2009-09-09
TIANJIN TAIPU PHARMA SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

U.S. Patent US5614529 discloses the preparation method of febuxostat, but does not disclose the crystal data of the compound, and then Chinese patent CN1275126A discloses various crystals of febuxostat and their preparation methods, but does not disclose ethanol solvation of febuxostat Any structure-determining data for crystallization

Method used

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  • Febuxostat and drug combination thereof
  • Febuxostat and drug combination thereof
  • Febuxostat and drug combination thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] Preparation of febuxostat crystals:

[0127] Get 2 grams of febuxostat, dissolve in 60ml 95% ethanol, cool down, leave naturally, precipitate crystals, filter, dry to obtain 1.94 grams of febuxostat crystals, yield 85%, then carry out SXRD and X-ray powder diffraction measurement , see the result figure 1 , figure 2 , image 3 and Figure 3-1 .

[0128] Its single crystal X-ray diffraction (SXRD) data are as follows:

[0129] Monoclinic crystal system, 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)°, with 2859 independent diffraction points and unit cell volume: 886.8(3) Crystal density: 1.357mg / mm 3 ; The shape is needle-shaped, and the size is 0.18×0.10×0.04mm.

[0130] The X-ray powder diffraction results of febuxostat crystals are shown in image 3 and Figure 3-1 . Data are as follows:

[0131] Instrument: Rigaku D / MAX-2500 X-ray diffractometer

[0132] Target: Cu-Ka radiation ...

Embodiment 2

[0136] Preparation of febuxostat crystals:

[0137] Take 5 grams of febuxostat, add 300ml of 60% ethanol to dissolve it, cool down, let it stand naturally, precipitate crystals, filter, and dry to obtain 5.1 grams of febuxostat crystals, with a yield of 89.2%, and then carry out SXRD and X-ray powder diffraction Measure, the result is with embodiment 1.

Embodiment 3

[0139] Preparation of febuxostat crystals:

[0140] Take 2 grams of febuxostat, add 45ml of absolute ethanol to dissolve it, cool down, let it stand naturally, precipitate crystals, filter, and dry to obtain 1.83 grams of febuxostat crystals, with a yield of 80.0%, and then perform SXRD and X-ray powder diffraction Measure, the result is with embodiment 1.

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Abstract

The invention relates to Febuxostat and a drug combination thereof, wherein the Febuxostat is Febuxostat crystal, belonging to monoclinic system, the space group of the crystal is P2 (1), and cell parameters comprise a=4.7179 (9), b=17.813 (4), c=10.690 (2), alpha=gamma=90 degrees, and beta=99.20 (3) degrees; and the cell volume is 886.8(3) <3>. In addition, the invention also relates to a drug composition containing the Febuxostat crystal and a preparation method of the crystal, and simultaneously the invention further discloses application of the Febuxostat crystal in treating hyperuricemia comprising primary and secondary hyperuricemia, acute and chronic gout, gouty arthritis, gouty nephropathy and renal calculus which are caused by the hyperuricemia.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and relates to novel febuxostat and its pharmaceutical composition, more specifically to febuxostat crystals, pharmaceutical compositions containing the crystals and their application in drugs for treating hyperuricemia . Background technique [0002] In recent years, with the change of people's dietary structure, the extension of life expectancy and the emphasis on gout, the incidence of gout has been increasing year by year, and it tends to be younger. Gout is mainly a disease caused by purine metabolic disorders. Its clinical features are hyperuricemia and the resulting gout, acute arthritis recurrent attacks, tophi deposition, tophi chronic arthritis and joint deformities and kidney disease. Cause chronic interstitial nephritis and uric acid kidney stone formation. The occurrence of gout is due to the excessive production of uric acid in the body and the decline in the ability of the...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P19/06A61P19/02A61P13/12
Inventor 赵健周学福魏文涛
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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