12 results about "Agomelatine" patented technology

FIELD: psychiatry; narcology.SUBSTANCE: used to stabilize remission of alcohol dependence in patients with comorbid depression. After the withdrawal state with alcohol dependence syndrome and comorbid depressive disorder has been relieved, the patient takes agomelatine orally at a dosage of 25 mg once a day daily for 12 weeks.EFFECT: method is accessible and allows for stabilizing remission in patients with alcohol dependence syndrome and depressive disorder.1 cl

The application provides a synthesis method of agomelatine. The starting material I is reacted with SOCl2 to obtain acyl chloride under the action of a solvent A, and then reacted with NH4OH to obtain intermediate I; the intermediate I is reacted with (CF3CO)2O under the action of a solvent B and triethylamine to obtain intermediate II through dehydration; the intermediate II is subjected to catalytic hydrogenation reaction with Raney Ni and H2 under the action of a solvent C to obtain intermediate III; the intermediate III is reacted with HCl under the action of a solvent D to obtain intermediate IV; and the intermediate IV is condensed with CH3COCl under the action of a solvent E and Cs2CO3 to obtain agomelatine. The method is simple in operation, mild in reaction condition, high in yield, low in cost, friendly to the environment, and suitable for industrial large-scale production of agomelatine.

The present invention relates to the use of agomelatine (or a prodrug or salt thereof) in the treatment of severe depression or bipolar affective disorder, comprising selecting a patient who will benefit most from agomelatine.

New co-crystal of agomelatine composed of: agomelatine, or N-[2-(7-methoxy-1naphthyl)ethyl]acetamide of formu1a (I)and - an organic acid, and a pharmaceutical composition comprising thereof for treating disorders of the melatoninergic system

This invention relates to an agomelatine microemulsion, a microemulsion gel, and a method for preparing the same, belonging to the field of pharmaceutical formulation. The agomelatine microemulsion comprises agomelatine and a drug carrier, the drug carrier including an emulsifier, a co-emulsifier, an oil phase, and an aqueous phase; the agomelatine microemulsion gel comprises an agomelatine microemulsion and a gel matrix. The agomelatine microemulsion and microemulsion gel of this invention exhibit good stability, high bioavailability, and good clinical safety, and the preparation process is simple and easily scaled up for industrial production.

The application relates to the technical field of pharmaceutical preparations, and discloses an agomelatine inhalant as well as a preparation method and application thereof. The agomelatine inhalant provided by the application comprises agomelatine or a pharmaceutically acceptable salt thereof in a form capable of being inhaled or capable of being changed into a form capable of being inhaled after being excited. From the aspect of synergism, the inhalant can avoid first-pass metabolism by changing a drug administration route, significantly improve bioavailability, and realize rapid effect by directly entering blood from the lung; from the aspect of attenuation, the inhalant can greatly reduce a drug usage amount to achieve a same treatment effect as a tablet, significantly reduce occurrence of drug toxic and side reactions, and significantly reduce liver toxicity by avoiding liver metabolism.

The present application provides a transdermal patch of agomelatine and a preparation method thereof. Specifically, the transdermal patch of agomelatine comprises (a) a backing layer, (b) an adhesive matrix layer and (c) a protective layer, wherein the adhesive matrix layer contains agomelatine and an adhesive matrix, and optionally further comprises a penetration enhancer. The transdermal patch of agomelatine prepared by the method has a fast transdermal absorption rate, a high transdermal absorption amount, and the characteristics of stability, high efficiency, good uniformity and low irritation, and the preparation method is simple.

This invention belongs to the field of pharmaceutical formulation technology, specifically relating to a transdermal absorption patch for agomelatine and its preparation method. The patch is a pressure-sensitive adhesive dispersion type patch, consisting of a backing layer, a drug-loaded pressure-sensitive adhesive layer, and an anti-adhesion layer. The drug-loaded pressure-sensitive adhesive layer comprises an agomelatine-organic acid eutectic mixture, a non-functionalized polyacrylate pressure-sensitive adhesive containing hexyl acrylate, and a transdermal absorption enhancer. The agomelatine-organic acid eutectic mixture accounts for 5.0-20 wt% of the total weight, the pressure-sensitive adhesive accounts for 70-94 wt%, and the transdermal absorption enhancer accounts for 0.5-10 wt%. The transdermal absorption patch for agomelatine provided by this invention enables 12-hour drug delivery, improves the low bioavailability and poor compliance of existing oral formulations, provides good mechanical adhesion, and enhances medication safety, accuracy, and patient compliance.

This invention relates to a method for preparing agomelatine, belonging to the field of pharmaceutical synthesis technology. To address the problems of long, unsafe, and low-yield existing routes, this invention provides a method for preparing agomelatine, comprising: reacting a compound of formula 8 with acetic anhydride to obtain the final product, compound 1 (agomelatine); further comprising reacting a compound of formula 4 with dimethyl sulfate in a mixed solvent of alcohol and water in the presence of an alkali metal hydroxide to obtain compound 5; subjecting compound 5 to hydrogenation reduction under the catalysis of borohydride to obtain compound 6; reacting compound 6 with benzylamine under the action of potassium tert-butoxide to obtain compound 7; and subjecting compound 7 to catalytic hydrogenation reduction under the catalysis of a palladium-containing catalyst to obtain compound 8. This invention features simple post-processing, easier recovery of the palladium catalyst, and high product yield, effectively improving reaction efficiency and safety.

The invention discloses a transdermal patch containing agomelatine as well as a preparation method and application of the transdermal patch. The transdermal patch comprises a polymer matrix layer, the polymer matrix layer comprises agomelatine as an active component, a water-insoluble crystallization inhibitor and a silicone pressure-sensitive adhesive, preferably, based on the weight of the polymer matrix layer, the weight content of agomelatine is 0.5-9%, the weight content of non-water-soluble crystallization inhibitor is 0.5-9%, and the weight content of silicone pressure-sensitive adhesive is 0.5-9%. The weight content of the water-insoluble crystallization inhibitor is 0.5%-50%, and the weight content of the silicone pressure-sensitive adhesive is 20%-99%. The transdermal patch disclosed by the invention is good in medicine permeability and colloid application performance, good in stability and high in safety, and can be used for treating depression patients.

This invention relates to the use of a reduced number of electroencephalogram (EEG) channels for predicting those who would benefit from drug treatment (such as with agomelatine) in patients with a psychiatric disorder (such as depression), as well as to an electroencephalogram (EEG) device for recording EEG data at these EEG channels.