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Three crystal forms of 5-methyl-7-methoxy-isoflavone, preparation method thereof, medicine composition thereof and application

A technology of methoxyisoflavone and composition, which can be applied in directions such as drug combination, medical preparations containing active ingredients, antipyretics, etc., and can solve the problems of few reports and the like

Active Publication Date: 2013-07-10
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 1979, 5-methyl-7-methoxy isoflavone has applied for a patent [see US Patent: 4163746], but there have been fewer related reports since then

Method used

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  • Three crystal forms of 5-methyl-7-methoxy-isoflavone, preparation method thereof, medicine composition thereof and application
  • Three crystal forms of 5-methyl-7-methoxy-isoflavone, preparation method thereof, medicine composition thereof and application
  • Three crystal forms of 5-methyl-7-methoxy-isoflavone, preparation method thereof, medicine composition thereof and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] 5-methyl-7-methoxyisoflavone crystal type A sample preparation method 1:

[0096] The preparation method of 5-methyl-7-methoxyisoflavone crystal type A sample is characterized in that the 5-methyl-7-methoxyisoflavone sample is completely dissolved and controlled at a normal temperature of 15 to 25°C using a methanol solvent. The solvent in the sample was quickly filtered or evaporated to dryness by vacuum filtration or rotary evaporation at a temperature of 45°C, and the sample was dried to finally prepare a crystalline type A solid sample of 5-methyl-7-methoxyisoflavone.

[0097] 5-methyl-7-methoxyisoflavone crystal type A sample preparation method 2:

[0098] The preparation method of 5-methyl-7-methoxyisoflavone crystal type A sample is characterized in that the mixed solution is prepared by using methanol and ethanol at a ratio of 3:1, and then the 5-methyl-7-methoxyisoflavone is mixed with The 7-methoxyisoflavone sample is completely dissolved, the temperature is ...

Embodiment 2

[0101] 5-methyl-7-methoxyisoflavone crystal type B sample preparation method 1:

[0102] The preparation method of 5-methyl-7-methoxyisoflavone crystal type B sample is characterized in that the 5-methyl-7-methoxyisoflavone sample is firstly mixed with tetrahydrofuran or dichloromethane solvent at a normal temperature of 15-25°C. Completely dissolve, control the temperature at 45°C, quickly filter or evaporate the solvent in the sample to dryness by vacuum filtration or rotary evaporation, and then dry the sample to finally prepare crystal B of 5-methyl-7-methoxyisoflavone type solid samples.

[0103] 5-methyl-7-methoxyisoflavone crystal type B sample preparation method 2:

[0104]The preparation method of 5-methyl-7-methoxyisoflavone crystal type B sample is characterized in that first dichloromethane is added to ethyl acetate at a ratio of 1:1 to prepare a mixed solution, and then 5 -Methyl-7-methoxyisoflavone sample is completely dissolved, the temperature is controlled a...

Embodiment 3

[0107] 5-methyl-7-methoxyisoflavone crystal type C sample preparation method 1:

[0108] The preparation method of 5-methyl-7-methoxyisoflavone crystal type C sample is characterized in that the solid sample of 5-methyl-7-methoxyisoflavone crystal type A is used as the preparation raw material, and the preparation method is high-temperature melting and quenching The process obtains 5-methyl-7-methoxyisoflavone crystal type C solid substance.

[0109] 5-methyl-7-methoxyisoflavone crystal type C sample preparation method 2:

[0110] The preparation method of 5-methyl-7-methoxyisoflavone crystal type C sample is characterized by firstly using n-butanol solvent to completely dissolve the 5-methyl-7-methoxyisoflavone sample at room temperature at 15-25°C , and then adopt cold spray method to quickly prepare and obtain 5-methyl-7-methoxyisoflavone crystal type C solid substance.

[0111] Problems that need to be explained: Since there are 19 single organic solvents used to prepare...

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Abstract

The invention discloses a crystal form B of 5-methyl-7-methoxy-isoflavone, a preparation method thereof, a medicine composition thereof and application. Concretely, the invention discloses that a 5-methyl-7-methoxy-isoflavone compound has the crystal form B in a solid state; the invention relates to the preparation method of the samples of the crystal form B; and the invention relates to the application of various preparations and the medicine composition which are prepared and developed by using the substances of crystal form of 5-methyl-7-methoxy-isoflavone as active ingredients in the preventive treatment of cardiovascular and cerebrovascular diseases, nervous system diseases, osteoporosis, inflammation, metabolic diseases and other diseases. The molecule formula of the 5-methyl-7-methoxy-isoflavone is shown below.

Description

technical field [0001] The present invention relates to the discovery that 5-methyl-7-methoxyisoflavone has three forms of crystal A, crystal B and crystal C in a solid state; and relates to the invention of a preparation method for samples of the three crystal forms. The present invention also relates to the application of different crystal forms of 5-methyl-7-methoxyisoflavone in the preparation of medicines for preventing and treating cardiovascular and cerebrovascular diseases, nervous system diseases, osteoporosis, metabolic diseases, inflammation and other diseases . Background technique [0002] 5-Methyl-7-methoxyisoflavone is a derivative of ipriflavone, and its systematic chemical name is 5-Methyl-7-Methoxyiso-flavone. The molecular structure is as follows: [0003] [0004] Studies have shown that the pharmacological activities of the two are similar, but 5-methyl-7-methoxyisoflavone has stronger activity, which can be used to prevent bone loss and treat bone d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/36A61K31/352A61P9/00A61P29/00A61P3/00A61P19/10
Inventor 杜冠华吕扬安会梅孙岚应剑吕丽娟赵艳
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI