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Agomelatine transdermal patch and preparing method thereof

A transdermal patch and patch technology, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations containing active ingredients. It can solve adverse reactions, poor accuracy and uniformity of drug content, nano Porous silica is not easy to prepare and other problems, so as to achieve the effect of ensuring treatment and improving percutaneous penetration rate

Active Publication Date: 2019-08-23
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This technical solution needs to be realized in a specific three-dimensional network configuration system. Nanoporous silica is not easy to prepare, and the accuracy and uniformity of drug content are poor; its release curve can only show a continuous growth state, which is difficult Reaching the effective concentration in a short time and the subsequent concentration is too high is prone to adverse reactions, which does not meet the requirements of clinical practical application

Method used

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  • Agomelatine transdermal patch and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Dissolve 40g of agomelatine in 100mL of DMF, filter, and pour the filtrate into 3000mL of rapidly stirring distilled water at 25°C at room temperature. After adding, stir at room temperature, filter, wash the filter cake with distilled water, dry the product in vacuum at room temperature, and determine by HPLC method, the content of agomelatine crystals is greater than 99%. After grinding, sieve, the particle size of micronized Selected from 1μm-8μm.

[0036] The crystalline crystal uses Cu-Kα radiation, and the X-ray powder diffraction spectrum has characteristic diffraction peaks at 12.83, 13.86, 16.15, 18.57, 19.11, 20.87, 21.21 and 23.85 in terms of 2θ angle.

[0037] X-ray powder diffraction conditions:

[0038] Instrument: Rigaku D / MAX-2500 X-ray diffractometer; target: Cu-Kα radiation (λ=1.5405), 2θ=2-40°C; step angle: 0.04°C; calculation time: 0.5s; tube pressure: 40KV; Tube flow: 100mA; scanning speed: 8°C / min; filter: graphite monochromator; 2θ value error: ...

Embodiment 2

[0040] A preparation method of agomelatine transdermal patch, comprising the following preparation steps:

[0041] (1) Take by weighing the crystalline powder of the micronized agomelatine 100mg prepared in Example 1;

[0042] (2) Measure fucosterol, octanoic acid, 2-pyrrolidone and isopropanol at a volume ratio of 1:1:1:2, with a total volume of 5 mL. After mixing, ultrasonically mix for 15 minutes at an ultrasonic power of 150W; The powder of (1) was added to the mixture of fucosterol, octanoic acid, 2-pyrrolidone and isopropanol, and ultrasonically mixed for 45min under the ultrasonic power of 150W.

[0043] (3) Coating the dispersed microspheres on the polymer pressure-sensitive adhesive to obtain the patch; wherein, the hot-melt pressure-sensitive adhesive is heated to melt, and the dispersion prepared in the preceding steps is coated on the anti-aging Adhesive material PET film, dried at 70°C, and then compounded with the backing material flesh-colored double-elastic cl...

Embodiment 3

[0045]A preparation method of agomelatine transdermal patch, comprising the following preparation steps:

[0046] (1) Take by weighing the crystalline powder of the micronized agomelatine 100mg prepared in Example 1;

[0047] (2) Measure fucosterol, octanoic acid, 2-pyrrolidone and isopropanol at a volume ratio of 2:1:1:4, with a total volume of 10mL. After mixing, ultrasonically mix for 15min at an ultrasonic power of 150W; The powder of (1) was added into the mixture of fucosterol, octanoic acid, 2-pyrrolidone and isopropanol, and ultrasonically mixed for 60 minutes under the ultrasonic power of 150W.

[0048] (3) Coating the dispersed microspheres on the polymer pressure-sensitive adhesive to obtain the patch; wherein, the hot-melt pressure-sensitive adhesive is heated to melt, and the dispersion prepared in the preceding steps is coated on the anti-aging Adhesive material PET film, dried at 70°C, and then compounded with the backing material flesh-colored double-elastic c...

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Abstract

The invention belongs to the technical field of medical preparations, and particularly relates to an agomelatine transdermal patch and a preparing method thereof. The preparing method comprises the following steps of micronizing an agomelatine crystal of a specific crystal form; dispersing the micronized crystal into a mixture of fucosterol, octanoic acid, 2-pyrrolidone and isopropanol; coating amacromolecule pressure-sensitive adhesive with a product to obtain the patch. According to the agomelatine transdermal patch and the preparing method thereof, the transdermal absorption rate of agomelatine is high, the agomelatine absorption amount is high, the patch has the advantages of being stable, efficient, high in uniformity and low in irritation, and wide clinical application is facilitated.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an agomelatine transdermal patch and a preparation method thereof. Background technique [0002] Agomelatine, English name Agomelatine, common chemical name: N-[2-(7-methoxynaphthalene-1-yl)ethyl]acetamide, CAS number: 138112-76-2, its chemical structure is as follows : [0003] [0004] Agomelatine is a drug for the treatment of major depression in adults, and its oral dosage form (tablet) has been marketed in Europe under the trade name Valdoxan. Each tablet contains 25mg of agomelatine, and the initial dose of 1 tablet is prescribed at bedtime, and the dose can be increased to 2 tablets (50mg) as needed. Oral agomelatine bioavailability is only about 5%, with severe first-pass hepatic metabolism, mainly caused by cytochrome CYP1A2 of the P450 isoenzyme system, which leads to hydroxylation and demethylation of agomelatine Tin conjugated met...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/28A61K47/12A61K47/22A61K47/10A61K31/165A61P25/24
CPCA61K9/7023A61K31/165A61K47/10A61K47/12A61K47/22A61K47/28A61P25/24
Inventor 贾文强黄伟堂张倩立
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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