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N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide and compound thereof

A technology of composition and crystal form, applied in the direction of drug combination, carboxylic acid amide separation/purification, organic active ingredients, etc., can solve problems such as weight change, side effects, sexual dysfunction, etc., and achieve the effect of adjusting sleep rhythm

Active Publication Date: 2010-07-14
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The mechanism of action of agomelatine is completely different from that of commonly used antidepressants such as selective serotonin reuptake inhibitors (SSRI) and serotonin-norepinephrine reuptake inhibitors (SNRI): SSRI and SNRI antidepressants achieve antidepressant efficacy by increasing the concentration of serotonin, but this also brings many side effects, such as weight change, sexual dysfunction, withdrawal syndrome, etc.

Method used

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  • N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide and compound thereof
  • N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide and compound thereof
  • N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide and compound thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Add 18.5 g of agomelatine to the reaction flask, add 37 ml of isopropanol, stir, heat to reflux until dissolved, add 185 ml of n-hexane after cooling slightly, stir to room temperature, stand for crystallization, filter, and dry to obtain a solid 14.8g.

[0038] The X-ray diffraction pattern of this crystalline powder is shown in figure 1 . Instrument model and measurement conditions: Rigaku D / max2500 diffractometer; CuKa 40Kv 100mA; 2θ scanning range: 0-50°;

[0039] The high performance liquid chromatography (HPLC) figure of this crystalline powder is shown in Figure 4 .

[0040] The thermal analysis results of the crystalline powder are shown in image 3 .

Embodiment 2

[0042] Granules containing a new crystal form of agomelatine

[0043] Prescription: 30 grams of agomelatine in new crystal form, 700 grams of lactose, 30 grams of crospovidone, 100 grams of microcrystalline cellulose, 40 grams of hydroxypropyl methylcellulose, appropriate amount of distilled water, made into 1000 bags .

[0044] Process: Mix raw and auxiliary materials, pass through 80-mesh sieve, mix with other materials, make soft material with distilled water, granulate, dry at low temperature, and then pack into granules.

Embodiment 3

[0046] Capsules containing a new crystal form of agomelatine

[0047] Prescription: 4 grams of agomelatine in the new crystal form, 150 grams of spray-dried lactose, made into 1000 capsules.

[0048]Process: After mixing the new crystal form of agomelatine and spray-dried lactose, the capsules are filled.

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Abstract

The invention relates to a new crystal form of N-[2-(7-methoxyl-1-naphthyl)ethyl]acetamide (agomelatine), a preparation method of the new crystal form, a medicine including the new crystal form, and an application of the pharmaceutical composition in the medicine treating the depression.

Description

technical field [0001] The present invention relates to a new crystal form of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide (Agomelatine, agomelatine), a preparation method of the new crystal form and a method containing the new crystal form Application of the medicament and the pharmaceutical composition in the medicament for treating depression. Background technique [0002] Agomelatine is the world's first melatonin receptor agonist antidepressant. It is both a melatonin receptor agonist and a 5-hydroxytryptamine 2C (S-HTx) receptor antagonist. It has the functions of antidepressant, anti-anxiety, regulating sleep rhythm and regulating biological clock. It is clinically used to treat depression. [0003] Agomelatine is a new breakthrough in the field of depression treatment. Its innovation lies in its unique mechanism of action. It is the world's first melatonin 1，2 (MT 1 MT 2 ) receptor agonist, but also five serotonin 2c (5HT2c) receptor antagonist. The mechanism o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/18C07C231/24A61K31/165A61P25/24
Inventor 严洁
Owner TIANJIN HANKANG PHARMA BIOTECH
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