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Favipiravir medicinal conjugate and application thereof to preparation of antiviral medicinal preparation

A technology of favipiravir and conjugates, which is applied in the field of pharmaceutical conjugates, can solve the problems of limiting the bioavailability of favipiravir and the development and application of related dosage forms, the research blanks of drug combination and crystal form, etc., and achieve The effect of low production cost, strong operability and easy operation

Active Publication Date: 2021-03-26
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since Favipiravir was officially launched in 2014, the main application form after the launch is tablets, and the research on its drug combination and crystal form is still relatively blank
And Favipiravir can only be slightly soluble in aqueous solution, which also obviously limits the bioavailability of Favipiravir and the development and application of related dosage forms

Method used

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  • Favipiravir medicinal conjugate and application thereof to preparation of antiviral medicinal preparation
  • Favipiravir medicinal conjugate and application thereof to preparation of antiviral medicinal preparation
  • Favipiravir medicinal conjugate and application thereof to preparation of antiviral medicinal preparation

Examples

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Embodiment 1

[0063] This embodiment provides a method for preparing favipiravir-theophylline drug co-crystal based on the solution method: accurately weigh 15.71 mg (0.1 mmol) of favipiravir raw material, 18.016 mg (0.1 mmol) of theophylline raw material, and Next, put the two weighed raw materials into a cleaned glass bottle (volume: 20ml), add an appropriate amount of ethanol until the drug is fully dissolved, the solution is clear, and the opening of the glass bottle is placed at room temperature and evaporated in a fume hood. Completely obtain the co-crystal drug of favipiravir and theophylline.

Embodiment 2

[0065] This embodiment provides another method for preparing favipiravir-theophylline drug co-crystal based on the solution method: Weigh 15.71mg (0.1mmol) of favipiravir raw material and 18.016mg (0.1mmol) of theophylline raw material, at room temperature Next, put the two weighed raw materials into a clean glass bottle (volume: 15ml), add 5mL of ethanol (other solvents include water, methanol, ethanol, acetone, acetic acid, ethyl acetate, acetonitrile, trifluoroethanol, isopropanol, n-butanol, chloroform, dichloromethane, chloroform, carbon tetrachloride, hexane tetrahydrofuran, dimethyl sulfoxide, N,N-dimethylformamide, or combinations thereof), the Put the glass bottle with the solution in a 65°C oil bath, add the cleaned magnets, and dissolve the drug fully at a speed of 360r / m, and it will appear as a clear solution, then place it at room temperature, cool down and crystallize after a period of time Afterwards, the co-crystal drug of Favipiravir and theophylline will be ...

Embodiment 3

[0067] In this embodiment, a method for preparing favipiravir-theophylline drug co-crystal based on grinding method is provided: accurately weigh 47.13 mg (0.3 mmol) of favipiravir raw material and 54.048 mg (0.3 mmol) of theophylline raw material, The sample is placed in a grinding bowl, Retsch MM200 grinding instrument, the frequency is 25Hz, grinding for 30 minutes, grinding without adding solvent or adding solvent (including water, methanol, ethanol, acetone, acetic acid, ethyl acetate, acetonitrile, trifluoroethanol, iso Propanol, n-butanol, chloroform, dichloromethane, chloroform, carbon tetrachloride, hexane tetrahydrofuran, dimethyl sulfoxide, N,N-dimethylformamide, or a combination of grinding aids can be obtained eutectic product.

[0068] For the favipiravir-theophylline cocrystal obtained in this embodiment, use an X-ray powder diffractometer, produced by Bruker, Germany, model D8 Advance, Cu-kα, tube voltage 40kV, tube current 40mA, step size 0.08, scan Range 10-...

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Abstract

The invention particularly relates to a favipiravir medicinal conjugate and an application thereof to preparation of an antiviral medicinal preparation. Favipiravir is a broad-spectrum antiviral drugwith a good prospect, but the favipiravir is poor in water solubility and low in bioavailability. The invention provides a medicinal conjugate form of the favipiravir, and theophylline and piperazineare adopted as forming substances of eutectic crystals and salt, so that the solubility of the favipiravir in water is remarkably improved, and a new research thought is provided for development of afavipiravir drug combined application mode and dosage forms.

Description

technical field [0001] The invention belongs to the technical field of medicinal conjugates, and specifically relates to a co-crystal of favipiravir and theophylline, a salt of fapilavir and piperazine, and a preparation method of the medicinal conjugate, comprising the drug The pharmaceutical composition of the conjugate and its application in antiviral pharmaceutical preparations. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Favipiravir (English name: favipiravir, Chinese name: 6-fluoro-3-hydroxypyrazine-2-carboxamide) is a broad-spectrum antiviral drug preparation developed by Fukuyama Chemical in Japan. In March 2014, it was approved in Japan for the treatment of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K31/4965A61K31/522A61K31/495A61P11/00A61P31/12A61P31/16A61P11/08C07D241/24C07D295/027C07D473/08
CPCA61K31/4965A61K31/522A61K31/495A61P31/12A61K9/14A61P31/14A61P31/20A61K2300/00Y02A50/30
Inventor 王蕾王新园陶绪堂谢冠英宋淑虹
Owner SHANDONG UNIV
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