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Agomelatine covered pellet and drug composition capable of being dispersed in mouth

A technology of agomelatine and coated pellets, which is applied in the direction of drug combination, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of low bioavailability of agomelatine, The pellets are prone to sticking and affecting the uniformity of coating, so as to achieve the effect of improving coating efficiency, good taste and not easy to stick

Active Publication Date: 2013-06-26
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, in the process of spraying the coating solution, the pellets tend to stick together, which affects the uniformity of the coating and reduces the coating efficiency, and it is easy to block the spray gun
[0012] Furthermore, pharmacokinetic studies have shown that the bioavailability of agomelatine administered orally relative to the parenteral route is very low and varies considerably within the same individual and between individuals Big

Method used

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  • Agomelatine covered pellet and drug composition capable of being dispersed in mouth
  • Agomelatine covered pellet and drug composition capable of being dispersed in mouth
  • Agomelatine covered pellet and drug composition capable of being dispersed in mouth

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: Preparation of orally disintegrating tablet sample 1 containing agomelatine

[0054] Preparation prescription of orally disintegrating tablets:

[0055]

[0056]

[0057] Preparation Process:

[0058] Weigh the prescribed amount of agomelatine and various auxiliary materials, pass through a 60-mesh sieve, and mix uniformly by equal-volume incremental method, then add lubricant talcum powder, mix well, and directly compress into tablets to obtain the product.

Embodiment 2

[0059] Example 2: Preparation of orally disintegrating tablet sample 2 containing agomelatine

[0060] (1) Prescription with Pill Heart:

[0061]

[0062] Wherein, each percentage in the dosage refers to the percentage of the component weight to the total weight of the pill-containing core (that is, the total weight of agomelatine, polyvinylpyrrolidone, and blank core). A similar understanding can also be made in the following embodiments.

[0063] Preparation of drug-containing pill cores: put blank pill cores into a fluidized bed to make them in a fluidized state, then pump the main drug solution dissolved in ethanol into the fluidized bed to prepare drug-containing pill cores.

[0064] (2) Prescription of coated pellets:

[0065] Coated pellets dosage

[0066] Pill Heart 83%

[0067] Eudragit E100 17%

[0068] 95% ethanol dosage is 9 times the weight of E100

[0069] Wherein, each percentage in the dosage refers to the percentage of the weight of the component to...

Embodiment 3

[0075] Example 3: Preparation of orally disintegrating tablet sample 3 containing agomelatine

[0076] (1) Prescription with Pill Heart:

[0077]

[0078] Preparation of drug-containing pill cores: put blank pill cores into a fluidized bed to make them in a fluidized state, then pump the main drug solution dissolved in ethanol into the fluidized bed to obtain drug-containing pill cores.

[0079] (2) Prescription of coated pellets:

[0080]

[0081] Preparation of coated micropills: Place the obtained drug-containing pill cores in a fluidized bed to make them in a fluidized state, then dissolve hypromellose in cold water and spray them on the drug-containing pellet cores to obtain coated micro-pellets. pill.

[0082] (3) Tablet prescription:

[0083]

[0084] Tablet preparation process:

[0085] Weigh various excipients in the prescribed amount, pass through a 60-mesh sieve, and mix them with agomelatine coated pellets in equal amounts, then add lubricant talcum ...

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Abstract

The invention belongs to the fields of pharmacology and pharmaceutical engineering and relates to an agomelatine covered pellet and a drug composition capable of being dispersed in the mouth. Concretely, the agomelatine covered pellet comprises an agomelatine main drug and a polyvinylpyrrolidone binding agent. According to the invention, agomelatine covered pellets are hardly adhered, so that pellet coating efficiency is improved and the problem that a spray gun is blocked is avoided; and the agomelatine-containing drug composition capable of being dispersed in the mouth can disintegrate quickly and is good in taste and high in bioavailability. The agomelatine-containing covered pellet and the drug composition capable of being dispersed in the mouth, which are provided by the invention, are easy to prepare, cost is reduced, and the agomelatine-containing covered pellet and the drug composition capable of being dispersed in the mouth are especially applicable to industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to agomelatine coated pellets and a pharmaceutical composition that can be dispersed in the mouth. Background technique [0002] Agomelatine has a chemical name of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, and its structural formula is shown in Formula I below. Agomelatine is a selective agonist of the melatonin receptor and 5-HT 2c Antagonist of receptors, these properties give it activity in the central nervous system, especially in major depression, seasonal affective disorder, sleep disturbance, cardiovascular disease, digestive system disease, insomnia and fatigue caused by jet lag, appetite Active in the treatment of disorders and obesity. [0003] [0004] Agomelatine, its preparation and use in therapy have been described in European patent applications EP 0447285 and EP 1564202. [0005] The advantages of orally disintegrating tablets are that they can rapidly inc...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K31/165A61K47/32A61K47/38A61P1/00A61P3/04A61P9/00A61P25/00A61P25/20A61P25/24
Inventor 梅兴国刘洪玉
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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