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Agomelatine crystal form B, preparation method thereof and medicinal composition containing same

A technology for agomelatine crystals and crystal forms, which is applied in the field of antidepressant drugs, can solve the problems of agomelatine product loss, cumbersomeness, poor reproducibility, etc., and achieves simple and easy operation, difficulty and cost of the method. The effect of reducing and improving the yield

Inactive Publication Date: 2010-06-09
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Abstract
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  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The preparation methods of agomelatine crystal form mentioned above are somewhat cumbersome. For example, heating and melting agomelatine, and then cooling to obtain the crystal product of the corresponding form requires the use of specific equipment; some reproducibility is not good, and there are uncertain factors For example, crystal form A, crystal form VI and their mixed crystals can be obtained by crystallization with isopropyl ether; some solvent recrystallization methods will cause agomelatine product loss, which greatly increases the difficulty and cost of industrial mass production

Method used

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  • Agomelatine crystal form B, preparation method thereof and medicinal composition containing same
  • Agomelatine crystal form B, preparation method thereof and medicinal composition containing same
  • Agomelatine crystal form B, preparation method thereof and medicinal composition containing same

Examples

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Effect test

Embodiment 1

[0029] Example 1: Preparation of agomelatine crystal form B

[0030] Add 100 g of agomelatine and 300 ml of ethanol to the reaction flask, heat and stir to dissolve. Cool the obtained agomelatine ethanol solution to 25±5°C, slowly add 2400ml of drinking water dropwise; after the dropwise addition, filter the precipitated crystals, and vacuum dry to obtain agomelatine 98.7g, yield: 98.7% .

[0031] The resulting product is measured by D / max-rA target X-ray diffractometer (copper to cathode) and expressed as follows with interplanar spacing d, Bragg 2θ angle, intensity and relative intensity (expressed as a percentage of the strongest ray):

[0032]

[0033]

[0034] Embodiment 2: Preparation of agomelatine crystal form B

[0035] Add 100 g of agomelatine and 500 ml of ethanol to the reaction flask, heat and stir to dissolve. Cool the obtained agomelatine ethanol solution to 25±5°C, slowly add 5000ml of drinking water dropwise; after the dropwise addition, filter the pr...

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Abstract

The invention relates to an agomelatine crystal form B, a preparation method thereof and a medicinal composition containing the same.

Description

technical field [0001] The present invention relates to antidepressant agomelatine crystal form B, its preparation method and its pharmaceutical composition. Background technique [0002] Agomelatine has a structural formula such as formula (I), and its chemical name is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide. [0003] [0004] Agomelatine is a melatonin 1, 2 (MT1, MT2) receptor agonist and also a 5-hydroxytryptamine 2c (5-HT2C) receptor antagonist, which can directly bind to the 5-HT2C receptor in the post-synaptic membrane. Body combination, so as to exert its antidepressant effect, and does not increase the concentration of 5-HT in the synapse, so there is no common side effect of serotonin reuptake inhibitor drugs and serotonin norepinephrine reuptake inhibitor drugs . Another unique target of the drug is the MT receptor. By stimulating the MT1 and MT2 receptors, it can adjust the patient's 24-hour rhythm and improve the patient's sleep quality, thereby promoting...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/18A61K31/165A61P25/24
Inventor 周世伟蹇锋
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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