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Three novel febuxostat medicament eutectic crystals and preparation method thereof

A febuxostat and drug technology is applied in the field of preparation of novel febuxostat organic drug co-crystals and drug co-crystals, and achieves the effects of good stability, high purity and simple and easy preparation method.

Active Publication Date: 2014-12-03
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At this stage, foreign research on drug co-crystals has gradually increased and deepened; while domestic research on it is still relatively small

Method used

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  • Three novel febuxostat medicament eutectic crystals and preparation method thereof
  • Three novel febuxostat medicament eutectic crystals and preparation method thereof
  • Three novel febuxostat medicament eutectic crystals and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Example 1: Add 3.16g (10mmol) of febuxostat and 1.22g (10mmol) of isonicotine to 100mL of acetonitrile, stir, heat to reflux to 85°C, the solution is clear, continue to stir for 0.5h, take it out at room temperature After 4 hours of complete precipitation, filter with suction and dry to obtain a light yellow solid powder, which is febuxostat organic drug eutectic 1.

Embodiment 2

[0082] Example 2: Add 0.316g (1mmol) of febuxostat and 0.122g (1mmol) of isonicotine to 30mL of benzonitrile, stir, heat to reflux to 50°C, the solution is clear, continue to stir for 0.5h, then take it out at room temperature Stand still, and after 48 hours of complete precipitation, filter with suction and dry to obtain light yellow crystals, which are febuxostat organic drug eutectic 1.

Embodiment 3

[0083] Example 3: Add 0.316g (1mmol) of febuxostat and 0.122g (1mmol) of isonicotine to 40mL of benzyl nitrile, stir, heat to reflux to 70°C, the solution is clear, continue to stir for 0.5h, then take it out at room temperature Stand still, and after 48 hours of complete precipitation, filter with suction and dry to obtain light yellow crystals, which are febuxostat organic drug eutectic 1.

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Abstract

The invention discloses three novel febuxostat medicament eutectic crystals and a preparation method thereof. The invention discloses febuxostat organic medicament eutectic crystals 1, 2 and 3, the water solubility of the three febuxostat medicament eutectic crystals is improved compared with febuxostat, especially, a febuxostat-meglumine eutectic crystal and a febuxostat-arginine eutectic crystal are currently eutectic crystals improving febuxostat dissolubility to be highest. In addition, the three febuxostat eutectic crystals are high in purity, less in impurity content, good in stability, and incapable of generating transformation of crystal forms during production and storage of a preparation when being used as raw materials, and the stability maintenance of the crystal form of the preparation is a necessary condition for the stable quality of the preparation. The preparation method of the eutectic crystals is simple and convenient and easy, mild in conditions, easy to control, good in reproducibility, the large-scale industrial production is easily realized, the production cost is low, and the three novel febuxostat medicaments eutectic crystals and preparation method thereof have great business application values.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, in particular to three novel febuxostat organic drug co-crystals and a preparation method for the drug co-crystals. Background technique [0002] Drug co-crystals are based on the principle of supramolecular chemistry, that is, molecular recognition and supramolecular self-assembly through intermolecular synergy. The active pharmaceutical ingredient (API) self-assembles with a suitable cocrystal former (CCF) through hydrogen bonds, or non-covalent bonds with saturation and directionality (such as van der Waals forces of aromatic hydrocarbons or benzene rings, π- π conjugation and halogen bond) to form a new structure, that is, drug co-crystal. In November 2011, the FDA issued the "Guidance for Industry: Regulatory Classification of Pharmaceutical Cocrystals", pointing out that when a drug forms a cocrystal with an excipient, the drug cocrystal can be used as a "preparation inter...

Claims

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Application Information

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IPC IPC(8): C07D277/56C07D213/81C07C279/14C07C277/08C07C215/10C07C213/08
CPCC07B2200/13C07C213/10C07C215/10C07C277/08C07C279/14C07D213/81C07D277/56
Inventor 吴素香康艳蕾胡秀荣
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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