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Ingavirin polymorph and its preparation method

A polymorph, ingavirine technology, which is applied in the field of polymorphs of ingavirine and its preparation, can solve the problem of affecting drug dissolution rate, affecting drug fluidity, tableting hardness, tablet weight difference and content uniformity Sexual and physical stability, affecting drug activity, etc.

Inactive Publication Date: 2013-11-06
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The polymorphic form of a drug is of great significance to the physical and chemical properties, bioavailability, and quality and process of the preparation. For example, the difference in physical and chemical properties between different crystal forms of a drug affects the stability of the drug. There may be large differences in availability, which will have a great impact on the preparation and seriously affect the activity of the drug
Because different crystal forms affect the dissolution rate of drugs, and the difference in surface free energy of different crystal forms causes different binding forces between crystal particles, which affects the fluidity of the drug, tablet hardness, tablet weight difference, content uniformity and physical properties. stability

Method used

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  • Ingavirin polymorph and its preparation method
  • Ingavirin polymorph and its preparation method
  • Ingavirin polymorph and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: Preparation of ingaverine crystal form A

[0058] Dissolve 2 g of ingavirin solid in 14 mL of water, add 60 mL of acetone, a white solid precipitates out, stir in an ice bath for 2 h, filter, and wash the filter cake twice with acetone to obtain 1.4 g of ingavirin crystal form A. Yield: 70%.

Embodiment 2

[0059] Embodiment 2: Preparation of ingaverine crystal form A

[0060] Add 2.98g of crude ingavirin and 50mL of methanol into the reaction kettle, add 25mL of triethylamine dropwise with stirring until the solid dissolves, then slowly add 360mL of ethyl acetate, cool down to 0°C, stir and crystallize for 2h, filter, and filter the cake Wash with 100 mL of ethyl acetate, collect the filter cake, and dry under reduced pressure to obtain 1.94 g of white solid, which is Ingavirine Form A.

Embodiment 3

[0061] Embodiment 3: Preparation of ingavirine crystal form B

[0062] Dissolve 2 g of ingavirin solid with 28 mL of water / ethanol (1:1), stir at room temperature for 24 h, filter, and wash the filter cake twice with ethanol to obtain 1.2 g of ingavirin crystal form B. Yield: 60%.

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Abstract

The invention belongs to the field of chemical pharmaceutical technology and relates to an ingavirin polymorph and its preparation method. The invention aims to provide the ingavirin polymorph in allusion to insufficiencies existing in the prior art. The invention provides ingavirin polymorphs A and B which have excellent physicochemical properties and good stability and are used in the research on in vivo study of ingavirin. Meanwhile, the invention provides a preparation method of the polymorphs A and B.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy, and relates to a polymorph of ingavirin and a preparation method thereof. Background technique [0002] Influenza virus, referred to as influenza virus, is an RNA virus that causes influenza in humans and animals. In taxonomy, influenza virus belongs to the Orthomyxoviridae family. It can cause acute upper respiratory tract infections and rapidly spread through the air. There are often periodic pandemics around the world. Human influenza viruses are divided into three types, A (A), B (B), and C (C), which are the pathogens of influenza (flu). Among them, the antigenicity of influenza A virus is easy to mutate, causing worldwide pandemics many times. [0003] Ingavirin (ingavirin, chemical name: 5-((2-(1 hydrogen-imidazol-4-yl) ethyl) amino)-5-oxopentanoic acid) is an effective drug against influenza virus and adenovirus infection. drug. Ingavirin is a non-toxic, broad-spectrum antiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/64
Inventor 吴勇朱义王一茜
Owner SICHUAN BAILI PHARM CO LTD
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