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Anti-fibrosis drug pirfenidone crystal forms and preparation method thereof

A technology of pirfenidone and anti-fibrosis, which is applied in the field of anti-fibrosis drug pirfenidone crystal form and its preparation, can solve the problems of no pirfenidone crystal form, etc., and achieve stable chemical and physical properties, crystal particles Uniform, easy-to-manufacture effect

Inactive Publication Date: 2016-08-31
HENAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this patent document only discloses a crystal form of pirfenidone, and there are no more relevant records about the crystal form of pirfenidone

Method used

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  • Anti-fibrosis drug pirfenidone crystal forms and preparation method thereof
  • Anti-fibrosis drug pirfenidone crystal forms and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Put 10g of pirfenidone in a 100mL two-necked flask, add 60mL of ethanol solution with a volume fraction of 10%, heat and stir in an oil bath until the raw material is completely dissolved, stop heating after the raw material is completely dissolved, and gradually cool down to 0-5°C Set aside for two hours, filter, and dry under normal pressure at 50° C. for 12 hours to obtain pirfenidone crystal form II powder.

Embodiment 2

[0022] Put 10g of pirfenidone in a 100mL two-necked flask, add 40mL of absolute ethanol, heat and stir in an oil bath until the raw materials are dissolved, stop heating after the raw materials are completely dissolved, gradually cool down to 0-5°C and let stand for two hours, filter, Drying at 50° C. for 12 hours under normal pressure with forced air to obtain the powder of pirfenidone crystal form III.

Embodiment 3

[0024] Put 10g of pirfenidone in a 500mL two-necked flask, add 50mL of ethyl acetate, stir at room temperature until the raw material is completely dissolved, gradually add 300mL of n-heptane dropwise under stirring, and keep warm at 0-5°C for 8 hours after the dropwise addition Filtrate, and dry at 50° C. under normal pressure for 12 hours to obtain the powder of pirfenidone crystal form III.

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Abstract

The invention discloses anti-fibrosis drug pirfenidone crystal forms and a preparation method thereof, and belongs to the technical field of anti-fibrosis drug pirfenidone. The technical scheme includes that the anti-fibrosis drug pirfenidone crystal forms include a pirfenidone crystal form II and a pirfenidone crystal form III, and the preparation method for the pirfenidone crystal form II and the pirfenidone crystal form III is provided specifically. The prepared pirfenidone crystal form II and the prepared pirfenidone crystal form III have the advantages of stable chemical-physical property, uniform crystal grain, suitability for long-term storage, convenience in preparation manufacture and the like.

Description

technical field [0001] The invention belongs to the technical field of anti-fibrosis drug pirfenidone, and in particular relates to a crystal form of the anti-fibrosis drug pirfenidone and a preparation method thereof. Background technique [0002] Pirfenidone, English name: Pirfenidone, chemical name: 5-methyl-1-phenyl-2 (1H) pyridone is a white or off-white powdery solid, the chemical structural formula is: . Fibrotic diseases such as renal fibrosis, liver cirrhosis, and myocardial fibrosis are important diseases that seriously endanger human life and health. With global industrialization and changes in people's lives and diets, the incidence of fibrotic diseases is gradually increasing . Aiming at the pathogenesis of fibrosis, scholars at home and abroad have screened and studied a large number of anti-fibrosis drugs from different fields such as natural medicines, chemical drugs, biological agents and gene therapy, and found that pyridone compounds are a class of effe...

Claims

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Application Information

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IPC IPC(8): C07D213/64
CPCC07D213/64C07B2200/13
Inventor 杨守宁杨嬅嬿李伟杨林余绍宁
Owner HENAN NORMAL UNIV
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