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Febuxostat pharmaceutical co-crystal and preparation method thereof

A technology for febuxostat and medicine, which is applied in the field of febuxostat drug co-crystal and its preparation, and can solve problems such as inactivation of allopurinol

Inactive Publication Date: 2013-04-17
吉林三善恩科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, unlike allopurine, which can only inhibit the reduced xanthine oxidase, when the molybdenum active center in the enzyme undergoes self-oxidation, it will inactivate allopurinol

Method used

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  • Febuxostat pharmaceutical co-crystal and preparation method thereof
  • Febuxostat pharmaceutical co-crystal and preparation method thereof
  • Febuxostat pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Synthesis of co-crystals using febuxostat and isonicotinic acid:

[0028] Weighing:

[0029] The reactants were fed with febuxostat 20.00mg and p-isonicotinic acid 20.00mg. Accurately weigh 20.00 mg febuxostat and 20.00 mg isonicotinic acid with an analytical balance.

[0030] Dissolution of API:

[0031] Use a 5ml pipette to accurately measure 5ml of ethyl acetate into a 20ml transparent glass vial container, stir for 1 hour to dissolve all the solids, and the solution becomes a colorless clear liquid.

[0032] Solvent room temperature evaporation heat method:

[0033] After the solid is completely dissolved, take out the stirring bar, seal the mouth of the bottle with tin foil, prick a few small holes with a needle, and let it stand for volatilization. After about 6 days, a colorless transparent block crystal was precipitated in the bottle.

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PUM

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Abstract

The invention belongs to the technical field of a pharmaceutical co-crystal, and particularly relates to a novel febuxostat pharmaceutical co-crystal and a preparation method thereof. The space group of piracetam pharmaceutical co-crystal prepared by the invention is a monoclinic system, one isonicotinic acid molecule and two febuxostat molecules are combined together through a hydrogen bond respectively to form a basic structural unit of the febuxostat pharmaceutical co-crystal. A solvent selected in a preparation process of pharmaceutical co-crystal is ethyl acetate, and a solvent room temperature volatilization method is adopted. Due to a relatively low boiling point of the selected organic solvent, crystal is separated out during the process of solvent volatilization. The pharmaceutical co-crystal prepared by the invention inherits characteristics of traditional medicaments in preparing hyperuricemia of gout patients, and also has obvious change on solubility, stability and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a novel drug co-crystal of febuxostat and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supramolecular chemistry is a science that st...

Claims

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Application Information

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IPC IPC(8): C07D277/56C07D213/803
Inventor 罗亚楠张婷苏红敏
Owner 吉林三善恩科技开发有限公司
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