Copolymer containing amorphous agomelatine, and preparation method, pharmaceutical composition and application thereof
A technology of agomelatine and copolymers, which is applied in the field of preparation of drugs for the treatment of depression, can solve problems such as agomelatine research reports, drug withdrawal syndrome, and sexual dysfunction that have not been seen, and achieve Stable temperature and humidity, fast absorption and high bioavailability
Active Publication Date: 2012-10-10
TIANJIN INSTITUTE OF PHARMA RESEARCH
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- Abstract
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Problems solved by technology
SSR I and SNR I achieve antidepressant efficacy by increasing the concentration of serotonin, but this brings many side effects, such as weight change, sexual dysfunction, withdrawal syndrome, etc.
However, there is no research report about amorphous agomelatine and its composition
Method used
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Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1-9
[0049] The following examples 1-9 are examples for preparing copolymers containing amorphous agomelatine
Embodiment 1
[0050] Embodiment 1: preparation by solvent method
[0051] Add 2 g of agomelatine and 10 g of povidone K25 into 100 ml of water, heat in a water bath at 60° C., ultrasonically dissolve to clarify, and distill to obtain a glass solution-like copolymer containing amorphous agomelatine.
Embodiment 2
[0052] Embodiment 2: preparation by solvent method
[0053] 2g agomelatine and 4g polyethylene glycol 6000 were added to 32ml of 80% (volume ratio) ethanol, heated in a water bath at 50°C, ultrasonically dissolved to clarify, rotary evaporated, dried, and pulverized to obtain an amorphous Copolymers of agomelatine.
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The invention provides a copolymer containing amorphous agomelatine. The detection of a sample of the copolymer by Differential Scanning Calorimetry (DSC) and X-ray powder diffraction shows that the sample has stable properties. The copolymer mainly comprises agomelatine raw material, carrier and solvent. The invention also provides a preparation method of the copolymer containing amorphous agomelatine, and the method has good reproducibility. The invention further provides a pharmaceutical composition containing the copolymer containing amorphous agomelatine and an application of the copolymer containing amorphous agomelatine in preparing medicines for treating depression.
Description
technical field [0001] The invention relates to a copolymer containing amorphous agomelatine and its preparation method, and the application of amorphous agomelatine as an active ingredient in the preparation of drugs for treating depression, which belongs to the pharmaceutical preparation technology field. Background technique [0002] Agomelatine (Agomelatine) obtained the marketing authorization of the European Union (EU) in February 2009 and is now on the market in some countries around the world for the treatment of depression in adult patients. [0003] The chemical name of agomelatine is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, which was first developed by the French Servier company. It is the only melatonin 1,2 (MT1MT2) receptor agonist, but also serotonin 2c (5HT2c) receptor antagonist drugs. Agomelatine has the effects of antidepressant, anti-anxiety, regulating sleep rhythm and regulating biological clock. At the same time, it has few adverse reactions, no ad...
Claims
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Patent Timeline
Login to View More IPC IPC(8): A61K47/48A61K31/165A61P25/00A61P25/20A61P25/22A61P25/24
Inventor 苏慕君臧可昕马超陈蔚潘毅陶勇靳朝东薛津
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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