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Novel febuxostat pharmaceutical co-crystal and preparation method thereof

A technology of febuxostat and medicine, applied in the field of novel febuxostat co-crystal and its preparation, to achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2013-04-24
JILIN INST OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug crystal form research and solid-state characterization of drugs are relatively mature and highly valued fields in the European and American pharmaceutical industry, but they are still in their infancy in the domestic pharmaceutical industry

Method used

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  • Novel febuxostat pharmaceutical co-crystal and preparation method thereof
  • Novel febuxostat pharmaceutical co-crystal and preparation method thereof
  • Novel febuxostat pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Synthesis of co-crystals using febuxostat and methanol:

[0026] Weighing: The reactant is fed according to 20.00 mg febuxostat. Accurately weigh 20.00 mg febuxostat with an analytical balance.

[0027] Dissolution of the raw material drug: Use a 5ml pipette to accurately measure 2ml of dichloromethane into a 20ml transparent glass vial container, and stir for 1 hour to dissolve almost all the solids. Then 3ml of methanol was added until all the solids were dissolved and the solution turned into a brownish-yellow clear liquid.

[0028] Solvent room temperature volatilization heating method: After the solid is completely dissolved, stir in a closed environment for 2 hours, then take out the stirring bar, seal the bottle mouth with tin foil, prick a few small holes with a needle, and let it stand for volatilization. After about 6 days, light yellow transparent block crystals precipitated in the bottle.

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals and specifically relates to a novel febuxostat pharmaceutical co-crystal and a preparation method thereof, wherein the atom O of hydroxyl in a methanol molecule serves as a hydrogen bond donor and the atom N of thiazole in a febuxostat molecule serves as a hydrogen bond receptor; and the hydrogen bond donor and the hydrogen bond receptor form the hydrogen bond so as to form the basic structure unit of the febuxostat co-crystal. The preparation method of the febuxostat pharmaceutical co-crystal provided by the invention is a room-temperature solvent evaporation method. The pharmaceutical co-crystal prepared by the method provided by the invention inherits the feature of the traditional raw material capable of treating the hyperuricemia of a gout patient, and is obviously improved in 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 febuxostat co-crystal 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 created the term "supramolecule" 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 studies comple...

Claims

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Application Information

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IPC IPC(8): C07D277/56
Inventor 罗亚楠曲晓姝杨艳艳连丽丽曹雪玲侯勇周广杰
Owner JILIN INST OF CHEM TECH
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