Preparation composite of agomelatine and preparation method thereof

Abstract

The invention relates to a preparation composite of agomelatine and a preparation method thereof. An agomelatine capsule is prepared from the following raw materials according to parts by weight: 25 parts of agomelatine, 50-70 parts of lactose, 35-45 parts of pregelatinized starch, 3-8 parts of sodium carboxymethyl starch, 55-65 parts of 5% povidone K30 aqueous solution and 1-2 parts of magnesiumstearate.

Description

technical field

[0001] The invention belongs to the field of pharmacy, and relates to a preparation composition of agomelatine and a preparation method thereof. Background technique

[0002] Agomelatine (agomelatine), chemical name N-[2-(7-methoxynaphthalene-1-naphthyl) ethyl] acetamide, its structural formula is as follows:

[0003]

[0004] Agomelatine has a dual action, not only an agonist of receptors of the melatoninergic system, but also an antagonist of 5HT2C receptors, and its properties make it active in the central nervous system, especially in major depression, seasonal Active in the treatment of affective disorders, sleep disorders, cardiovascular diseases, digestive disorders, jet lag-induced insomnia and fatigue, appetite disorders and obesity. It is the first melatonin-type antidepressant that is effective in the treatment of depression and improves sleep function.

[0005] At present, foreign companies have already launched agomelatine tablets on the mar...

Examples

Embodiment 1

[0055] Take agomelatine 25g, lactose 60g, pregelatinized starch 40g, carboxymethyl starch sodium 5g, 5% povidone K30 aqueous solution 65g, magnesium stearate 1g.

[0056] The preparation method of the above-mentioned agomelatine capsules comprises the following processing steps:

[0057] (1) Take the above parts by weight of agomelatine, lactose, pregelatinized starch, and sodium carboxymethyl starch and pass through an 80-mesh sieve;

[0058](2) Take Povidone K30 by weighing, add purified water (mass ratio 5:95) and stir to make 5% Povidone K30 aqueous solution by weight:

[0059] (3) Mix lactose, pregelatinized starch and sodium starch glycolate evenly, and then mix agomelatine with it.

[0060] (4) Add the prepared 5% povidone K30 aqueous solution as a binder and add to step (3) to make a soft material, pass through a 24-mesh sieve for granulation. Place in an oven at 55-65°C to dry to obtain dry granules.

[0061] (5) Pass the dry granules through a 20-mesh sieve for si...

Embodiment 2

[0065] Take agomelatine 25g, lactose 50g, pregelatinized starch 35g, carboxymethyl starch sodium 3g, 5% povidone K30 aqueous solution 55g, magnesium stearate 1g. 1,000 agomelatine capsules can be prepared, and each capsule contains 25 mg of the active ingredient agomelatine. All the other are with embodiment 1.

Embodiment 3

[0067] Take agomelatine 25g, lactose 70g, pregelatinized starch 45g, carboxymethyl starch sodium 8g, 5% povidone K30 aqueous solution 65g, magnesium stearate 2g. 1,000 agomelatine capsules can be prepared, and each capsule contains 25 mg of the active ingredient agomelatine. All the other are with embodiment 1.

technical field

[0001] The invention belongs to the field of pharmacy, and relates to a preparation composition of agomelatine and a preparation method thereof. Background technique

[0002] Agomelatine (agomelatine), chemical name N-[2-(7-methoxynaphthalene-1-naphthyl) ethyl] acetamide, its structural formula is as follows:

[0003]

[0004] Agomelatine has a dual action, not only an agonist of receptors of the melatoninergic system, but also an antagonist of 5HT2C receptors, and its properties make it active in the central nervous system, especially in major depression, seasonal Active in the treatment of affective disorders, sleep disorders, cardiovascular diseases, digestive disorders, jet lag-induced insomnia and fatigue, appetite disorders and obesity. It is the first melatonin-type antidepressant that is effective in the treatment of depression and improves sleep function.

[0005] At present, foreign companies have already launched agomelatine tablets on the mar...

Examples

Embodiment 1

[0055] Take agomelatine 25g, lactose 60g, pregelatinized starch 40g, carboxymethyl starch sodium 5g, 5% povidone K30 aqueous solution 65g, magnesium stearate 1g.

[0056] The preparation method of the above-mentioned agomelatine capsules comprises the following processing steps:

[0057] (1) Take the above parts by weight of agomelatine, lactose, pregelatinized starch, and sodium carboxymethyl starch and pass through an 80-mesh sieve;

[0058](2) Take Povidone K30 by weighing, add purified water (mass ratio 5:95) and stir to make 5% Povidone K30 aqueous solution by weight:

[0059] (3) Mix lactose, pregelatinized starch and sodium starch glycolate evenly, and then mix agomelatine with it.

[0060] (4) Add the prepared 5% povidone K30 aqueous solution as a binder and add to step (3) to make a soft material, pass through a 24-mesh sieve for granulation. Place in an oven at 55-65°C to dry to obtain dry granules.

[0061] (5) Pass the dry granules through a 20-mesh sieve for si...

Embodiment 2

[0065] Take agomelatine 25g, lactose 50g, pregelatinized starch 35g, carboxymethyl starch sodium 3g, 5% povidone K30 aqueous solution 55g, magnesium stearate 1g. 1,000 agomelatine capsules can be prepared, and each capsule contains 25 mg of the active ingredient agomelatine. All the other are with embodiment 1.

Embodiment 3

[0067] Take agomelatine 25g, lactose 70g, pregelatinized starch 45g, carboxymethyl starch sodium 8g, 5% povidone K30 aqueous solution 65g, magnesium stearate 2g. 1,000 agomelatine capsules can be prepared, and each capsule contains 25 mg of the active ingredient agomelatine. All the other are with embodiment 1.

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