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New crystalline form iii of agomelatine, a process for its preparation and pharmaceutical compositions containing it

A technology of crystal form and medicine, applied in the new crystal form III of N-[2-ethyl]acetamide: field, can solve problems such as no specific description

Inactive Publication Date: 2009-01-14
LES LAB SERVIER SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the document does not specify the conditions under which agomelatine exhibiting these properties can be obtained in a reproducible manner

Method used

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  • New crystalline form iii of agomelatine, a process for its preparation and pharmaceutical compositions containing it
  • New crystalline form iii of agomelatine, a process for its preparation and pharmaceutical compositions containing it
  • New crystalline form iii of agomelatine, a process for its preparation and pharmaceutical compositions containing it

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Form III of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide

[0019] Heat 100 g of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide in a ventilated incubator at 110°C until it melts completely, then cool slowly until crystallization. The obtained crystalline form III is characterized by the following powder X-ray diffraction pattern, which is measured using a Siemens D5005 diffractometer (copper to cathode), expressed in terms of interplanar distance d, Bragg 2θ angle, intensity and relative intensity (expressed as a percentage of the strongest ray) :

[0020]

Embodiment 2

[0021] Embodiment 2: pharmaceutical composition

[0022] Prepare a prescription for 1000 tablets, each containing a 25mg dose:

[0023] Compound of Example 1 ................................................ ......25g

[0024] Lactose monohydrate ................................................ ..........62g

[0025] Magnesium stearate.............................................. ..........1.3g

[0026] corn starch................................................ ..........26g

[0027] Maltodextrin mixture................................................ ......9g

[0028] Anhydrous colloidal silica................................................ ......0.3g

[0029] Sodium Starch Glycolate Type A ................................................ .......4g

[0030] Stearic acid................................................ ..........2.6g

Embodiment 3

[0031] Embodiment 3: pharmaceutical composition

[0032] Prepare a prescription for 1000 tablets, each containing a 25mg dose:

[0033] Compound of Example 1 ................................................ ......25g

[0034] Lactose monohydrate ................................................ ..........62g

[0035] Magnesium stearate.............................................. ..........1.3g

[0036] Povidone................................................ ................9g

[0037] Anhydrous colloidal silica................................................ ......0.3g

[0038] Sodium carboxymethyl cellulose............................................ ..........30g

[0039] Stearic acid................................................ ..........2.6g

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Abstract

Crystal form III of the compound of formula (I) and medicaments containing it, the crystal form being characterized by its powder X-ray diffraction pattern.

Description

technical field [0001] The present invention relates to the new crystal form III of agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I): [0002] [0003] Its preparation method and pharmaceutical composition containing it. Background technique [0004] Agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, has valuable pharmacological properties. [0005] It does have a dual profile, on the one hand, it is an agonist of receptors of the melatonergic system, on the other hand, it is a 5-HT 2C receptor antagonists. These properties make it active in the central nervous system, more particularly in severe depression, seasonal affective disorder, sleep disturbances, cardiovascular diseases, digestive disorders, insomnia and fatigue due to jet lag, appetite disturbances active in the treatment of obesity. [0006] Agomelatine, its preparation and its therapeutic use are described in European patent specification EP 0 447 285 . [0007] In view o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C233/18A61K31/165A61P25/00A61P25/24A61P25/18A61P9/00A61P1/00A61P25/20A61P3/04
CPCC07C2102/10C07C231/24C07C233/18C07C2602/10A61P1/00A61P15/00A61P15/08A61P17/00A61P25/00A61P25/06A61P25/08A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P3/00A61P3/10A61P35/00A61P3/04A61P37/00A61P43/00A61P5/06A61P9/00
Inventor G·科克雷尔J·里诺尔J-C·苏维
Owner LES LAB SERVIER SA
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