Medicine composition containing agomelatine

Abstract

The invention belongs to the technical field of medicine, and discloses a medicine composition containing agomelatine prepared form components of, by weight: 11% to 25% of agomelatine, 30% to 65% of lactose, 11% to 40% of starch, 8% to 15% of carboxymethylstarch sodium, 0.5 to 5% of stearic acid, 0.6% to 2% of magnesium stearate, and 0.5% to 5% of silicon dioxide. As a result of experiments, preparations prepared with the medicine composition provided by the invention provide a better dissolution rate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition containing agomelatine. Background technique [0002] Agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I): [0003] [0004] And its hydrates, crystalline forms and pharmaceutically acceptable acid or base addition salts have valuable pharmacological activity: agomelatine is a melatonin receptor agonist (MT1 and MT2 receptors) and 5-HT2C Antagonist, which makes it central nervous system active, especially in the treatment of major depression, seasonal affective disorder, sleep disturbances, cardiovascular diseases, digestive disorders, insomnia and fatigue due to jet lag, appetite disorders and obesity active. [0005] Agomelatine, its preparation and use in therapy have been described in European Patent Specifications EP0 447 285 and EP1 564 202 . [0006] CN1287780C discloses an orally dispersible pharmaceutic...

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Problems solved by technology

[0006] CN1287780C discloses an orally dispersible pharmaceutical composition containing agomelatine, which mainly exists in the form of tablets and is prepared by direct compression. The hardness of the tablets is 20 Newtons, and the disintegration in the oral cavity is The disintegration time is less than 3 minutes. This orally disintegrating composition may improve the bioavailability of agomelatine in the human body, but the direct and rapid disintegration in the oral cavity may lead to the rapid release of the bad taste of the drug and reduce the patient's health. Compliance, and to achieve rapid oral disintegration, the hardness of the tablet is generally relatively small, which brings difficulties to transportation and packaging

[0007] CN1981752A discloses an orally dispersible pharmaceutical composition for oromucosal or sublingual administration of agomelatine, the pharmaceutical composition uses and other accessories, It is a new type of compound made of 15% corn starch and 85% lactose monohydrate through spray drying-coagulation. This excipient needs to be imported, which is expensive and difficult to obtain relevant legal qualifications. It is not suitable for industrial production of preparations

[0008] CN101152143A discloses a pharmaceutical composition containing agomelatine. The method improves the biological activity of agomelatine in the human body by adding nonionic hydrophilic surfactants to the pharmaceutical composition of agomelatine. Utilization, this invention may improve the bioavailability of agomelatine in the human body, but long-term application or high-concentration use of surfactants may cause mucosal damage, and the bioavailability of agomelatine tablets currently produced The degree meets the requirements, adding non-ionic hydrophilic surfactants to the formulation will undoubtedly increase the production cost

[0009] CN101732296A discloses a pharmaceutical composition containing agomelatine. The method uses lactose, starch, sodium carboxymethyl starch and magnesium stearate. It is noteworthy that agomelatine is a poorly soluble drug and Poor fluidity, it is difficult to ensure the dissolution rate of the product in the actual production of preparations, and this method uses the method of equal increase to granulate, which is not suitable for large-scale production

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