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A kind of composite crystal, preparation method and application

A compound and crystal technology, applied in the field of chemical medicine, can solve the problem of not providing crystal structure data, etc., and achieve the effects of prolonging the onset time, delaying the dissolution rate, and reducing toxic and side effects

Active Publication Date: 2022-05-24
BEIJING INSTITUTE OF PETROCHEMICAL TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A new crystal form is reported in CN 107759529 A patent, but no crystal structure data is provided

Method used

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  • A kind of composite crystal, preparation method and application
  • A kind of composite crystal, preparation method and application
  • A kind of composite crystal, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] After mixing favipiravir with p-aminobenzoic acid in a molar ratio of 1:1, take about 2g of solids, add about 0.5 ml of ethyl acetate and manually grind in a mortar for 30 min. Samples are placed in a blast drying chamber and dried at 30 °C. The resulting product was XRD analyzed as a eutectic of favipiravir-p-aminobenzoic acid.

Embodiment 2

[0033] After mixing favipiravir and p-aminobenzoic acid in a molar ratio of 1:1, about 2g of solids were taken, 10ml of methyl tert-butyl ether was added, and magnetic stirring was stirred at room temperature for 72h to 96h. After the sample is filtered, the resulting solids are placed in a blast drying box and dried at 60 °C. The resulting solids were analyzed by XRD and showed that they were eutectic of favipiravir-p-aminobenzoic acid.

Embodiment 3

[0035] Take 0.6 g of p-aminobenzoic acid, add 50 ml of ethyl acetate, heat and dissolve. Add 0.456 g of favipiravir and stir for 2h. The solids were filtered and dried in a blast at 40 °C, and XRD analysis showed that they were eutectic of fapilabvir-p-aminobenzoic acid.

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Abstract

The invention discloses a compound crystal, a preparation method and an application belonging to the technical field of chemistry and medicine. The complex crystal is a co-crystal of favipiravir and p-aminobenzoic acid. The unit cell of the co-crystal belongs to the monoclinic system, the space group P21 / c, and the unit cell parameters are: α=γ=90°, β=92.578 (3)°. The equivalent solubility of favipiravir in the complex crystal provided by the invention has been reduced by about 50%, which helps to delay the dissolution rate of favipiravir, prolong the onset time of favipiravir, and reduce the toxicity of favipiravir. side effect.

Description

Technical field [0001] The present invention belongs to the field of chemical and pharmaceutical technology, particularly relates to a composite crystal, preparation methods and applications. Background [0002] 6-Fluoro-3-hydroxypyrazine-2-carboxamide (favipiravir, cas259793-96-9, Chinese fapiravir) and 4-aminobenzoic acid chemical structure as shown in formulas 1 and 2. [0003] [0004] 6-Fluoro-3-hydroxypyrazine-2-carboxamide is a toyama Chemical Co., Ltd. (Toyama Chemical Co., Ltd.) A pyrazine analogue drug was developed that was initially approved for the treatment of drug-resistant influenza. 6-Fluoro-3-hydroxypyrazine-2-carboxamide not only inhibits the replication of influenza A and B, but the drug also has greater promise in the treatment of avian influenza. There are current studies of fapiravir for the treatment of other deadly viral infections, such as Ebola, Lassa and COVID-19. [0005] In WO12043700A1 and WO12043696A1, the sodium salt of 6-fluoro-3-hydroxy-2-pyra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D241/24C07C229/60C07C227/42A61K31/4965A61P31/16
CPCC07D241/24C07C229/60A61P31/16C07B2200/13
Inventor 何运良张阗王学重周浩宇
Owner BEIJING INSTITUTE OF PETROCHEMICAL TECHNOLOGY
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