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Freeze-dried oral preparation containing agomelatine and preparation method thereof

An oral preparation and freeze-drying technology, applied in the field of pharmaceutical preparations, can solve the problems of difficulty in taking ordinary tablets, long absorption process time, slow drug release speed, etc., achieve pregastric absorption and water-free delivery, and improve compliance. , the effect of accelerating the dissolution rate

Active Publication Date: 2015-12-30
CHENGDU XINJIE HIGH TECH DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the BCS guidelines, agomelatine is considered as a BCS class II compound (low solubility and high permeability), therefore, it is not easy to disintegrate, and the release rate of the drug in the oral cavity is slow. If it completely depends on the gastric environment to make it dissolve And absorbed in the intestinal environment, this absorption process takes a long time and is not conducive to the patient's control effect in a very short time (about 30 minutes)
[0007] At the same time, due to the different conditions of depression patients, it may be difficult to take ordinary tablets, and they need to be taken with water during the taking process. If they are taken improperly, it may cause esophageal discomfort, affect the patient's mood, and have an impact on clinical treatment.

Method used

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  • Freeze-dried oral preparation containing agomelatine and preparation method thereof
  • Freeze-dried oral preparation containing agomelatine and preparation method thereof
  • Freeze-dried oral preparation containing agomelatine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] This example provides a lyophilized oral formulation containing agomelatine, the prescription of which is shown in Table 1 below.

[0043]

[0044] Table 1

[0045]The flavoring agent in the above prescription can be one of aspartame or anhydrous citric acid alone, and the dosage is 0.001mg~0.81mg. Preferably, the flavoring agent includes aspartame and anhydrous citric acid, wherein aspartame is located in the sweetness regulator, and anhydrous citric acid is used as the sourness regulator.

[0046] It is easy to understand that according to the actual use, the above-mentioned excipients of the freeze-dried preparation can also be replaced by other similar excipients, and the dosage of the above-mentioned excipients can be adjusted appropriately to meet the pharmaceutical dosage requirements of the components.

Embodiment 2

[0048] According to the prescription in Example 1, this implementation provides a preparation method of a freeze-dried oral preparation containing agomelatine, comprising the following steps:

[0049] A. Dissolve the prescribed amount of flavoring agent in 300ml of purified water, add the prescribed amount of freeze-dried skeleton proppant and binder, and stir until dissolved; then add agomelatine raw material, and continue to stir until dissolved Add purified water to make the volume to 500ml to obtain the medicinal solution;

[0050] B. The fully stirred medicinal solution in step A is left to stand, and degassed by ultrasound; the degassed medicinal solution is respectively packaged and poured into each aluminum foil blister mold, and heated at -40°C~ Quick-frozen and shaped at -120°C, then transferred to a freeze dryer for freeze-drying so that the moisture content was <2%, and a freeze-dried oral preparation was obtained.

[0051] The above-mentioned freeze-drying includ...

Embodiment 3

[0055] In this example, the quality evaluation of the freeze-dried oral preparation in Example 1 was carried out.

[0056] (1) Disintegration evaluation

[0057] In vitro disintegration ①: Put the product on a glass plane, add 1 drop of water (about 0.02ml) (37°C±0.5°C) at a distance of 0.5cm from the tablet surface of the product and time it accurately. The standard limit is no more than 15 seconds;

[0058] In vitro disintegration ②: Measured by (Chinese Pharmacopoeia 2015 Edition, Part IV General Rule 0921), the standard limit is no more than 10 seconds.

[0059] (2) Taste evaluation: 5 volunteers evaluated the taste, put the product on the tip of their tongues, observed the disintegration situation and recorded the oral disintegration time, whether there is a sandy feeling after complete disintegration, whether the sweet and sour taste is good, etc.

[0060] (3) Character evaluation: The surface of the product is required to be smooth; the packaging is completely stripped...

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Abstract

The invention provides a freeze-dried oral preparation containing agomelatine and a preparation method thereof and belongs to the field of medicinal preparations. The freeze-dried oral preparation is prepared from agomelatine in medicine dosage and freeze-dried preparation auxiliary materials. According to the preparation method, agomelatine and the auxiliary materials are prepared into the freeze-dried oral preparation through a freeze-drying method. Agomelatine and the freeze-dried preparation auxiliary materials are dissolved in purified water and then subjected to freeze drying, and then the freeze-dried oral preparation containing agomelatine is prepared. Due to the fact that the freeze-dried oral preparation can be quickly disintegrated in the oral cavity or the stomach, the dissolving-out speed of medicine is increased, absorption before the stomach and taking without water of agomelatine are achieved through mucous membrane transfer, the disintegration and absorption time of agomelatine is shortened, and therefore bioavailability and the compliance of clinic patients are improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried oral preparation containing agomelatine and a preparation method thereof. Background technique [0002] Agomelatine is a melatonin analog, the first melatonin receptor agonist, and a serotonin receptor antagonist. Animal experiments and clinical studies have shown that the drug has the functions of antidepressant, anti-anxiety, regulating sleep rhythm and regulating biological clock. At the same time, it has few adverse reactions, no adverse effects on sexual function, and no drug withdrawal reaction. This product is clinically used to treat severe depressive episodes in adults. [0003] The chemical name of agomelatine is N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide, and its chemical structural formula is as follows: [0004] . [0005] Agomelatine was developed by the French company Servier, and its tablets were approved for marketing in the Euro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/165A61K47/26A61K47/10A61K47/42A61K47/36A61P25/24A61P25/22A61P25/20
Inventor 蒲洪高红刘晓琳欧世荣
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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