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Agomelatine-containing medicinal composition for oral mucosa or sublingual administration

A technology for sublingual administration of agomelatine, which is applied to drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as high cost and complicated preparation process, and achieve low cost and excellent preparation method simple effect

Active Publication Date: 2012-07-18
CHENGDU KANGHONG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In view of the above-mentioned deficiencies in the prior art, the object of the present invention is to provide a oral mucosal or sublingual administration of agomelatine with simple preparation process, suitable for industrial production, low production cost, no irritation and good taste. The new preparation of agomelatine drug solves the shortcomings of complex preparation process and high cost of the existing oral mucosa administration agomelatine preparation. Therapeutics provide new options and fill gaps in the market

Method used

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  • Agomelatine-containing medicinal composition for oral mucosa or sublingual administration
  • Agomelatine-containing medicinal composition for oral mucosa or sublingual administration

Examples

Experimental program
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Effect test

Embodiment 1 to 7

[0084] The pharmaceutical composition was prepared by adopting agomelatine with different particle sizes, and the formula is shown in Table 7. Preparation method (wet granulation and tabletting): mix agomelatine with mannitol and cross-linked polyvinylpyrrolidone evenly, add an appropriate amount of 5% hypromellose for wet granulation, and mix the obtained dry granules with magnesium stearate, Mix micronized silica gel evenly, and press into tablets.

[0085] Table 7 Embodiment 1-7 (calculated by weight percentage)

[0086]

[0087]

[0088] Remarks: Add about 8g (0.4g) of 5% hypromellose solution per 100g of solid material, and the amount of hypromellose is not included in the formula.

[0089] Find 6 healthy volunteers to use, through oral mucosa and sublingual administration, evaluate its stimulation intensity and detect its dissolution rate. The results are shown in Table 8.

[0090] Table 8 embodiment 1-7 evaluation result

[0091]

[0092] Summary: It can be...

Embodiment 8 to 18

[0094] The choice of diluent has a certain influence on the irritation and dissolution rate of this product. It is known to those skilled in the art that soluble excipients such as mannitol, sorbitol, lactitol, sucrose, lactose, glucose, or insoluble excipients such as starch, dextrin, calcium sulfate and microcrystalline cellulose can be used as the ingredients of tablets. thinner. The inventor studies the situation of different adjuvants as the diluent of the present invention through sufficient experiments, and the results show that the diluent suitable for the pharmaceutical composition of agomelatine of the present invention can be any excipient commonly used for dilution in the pharmaceutical field. Excipients, including but not limited to one or more of the above-mentioned diluents.

[0095] The present invention is further illustrated by the following specific experiments: using the above composition formulations of different diluents (see Table 9 and Table 10), the p...

Embodiment 19-38

[0112] In addition to diluents, disintegrants, and lubricants, the pharmaceutical composition of the present invention may also contain other pharmaceutical excipients. The specific formulations are shown in Table 13 and Table 14. The particle size range of agomelatine used is 48 μm- 150 μm. The preparation method is as follows:

[0113] Step 1: crush the main drug, diluent, lubricant, disintegrant, flavoring agent, antioxidant, opacifier, penetration enhancer, and sieve for pretreatment.

[0114] Step 2: Mix the pretreated main drug, diluent, lubricant, disintegrant, flavoring agent, antioxidant, opacifier and penetration enhancer evenly;

[0115] Step 3: compress the uniformly mixed above-mentioned materials into tablets.

[0116] Table 13 Embodiment 19-29 (calculated in weight percentage)

[0117]

[0118] Note: the lactose used in Examples 22 and 24 is ground lactose; the lactose used in Example 29 is spray-dried lactose.

[0119] Table 14 Embodiment 30-38 (calculat...

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Abstract

The invention discloses an agomelatine-containing medicinal composition for oral mucosa or sublingual administration and a preparation method thereof. The medicinal composition consists of a main medicament of which the particle diameter is 48-250 mum and is preferably 48-150 mum, and medicinal auxiliary materials. The medicinal composition can be prepared through a simple preparation process without special production equipment, has low manufacturing cost, and is suitable industrial production; moreover, the use compliance of a patient is improved through the excitement of the taken medicament in an oral cavity; and the medicinal composition is absorbed directly through oral mucosa, so that the first pass effect of the conventional oral medicament is avoided, and the bioavailability is high.

Description

technical field [0001] The invention relates to a pharmaceutical composition of agomelatine, in particular to an agomelatine tablet which is mainly absorbed through oral cavity or sublingual mucosa and takes effect quickly and a preparation method thereof. Background technique [0002] The listing of agomelatine is a new breakthrough in the field of depression treatment. Its novelty lies in its unique mechanism of action. It is the world's first melatonin 1, 2 (MT1, MT2) receptor agonist, and also an antagonist of five serotonin 2c (5-HT2c) receptors. 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 ...

Claims

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Application Information

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IPC IPC(8): A61K31/165A61K9/20A61P25/24
Inventor 柯潇郑强王万
Owner CHENGDU KANGHONG PHARMA GRP
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