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Agomelatine-isonicotine eutectic crystal and compound and preparation method thereof

A technology of isonicotine and composition, which is applied in the field of agomelatine-isonicotine co-crystal and its composition and preparation, can solve the problem of poor water solubility of agomelatine crystal form and affect the drug effect , high production cost and other issues, to achieve the effect of easy preparation, easy control and low production cost

Inactive Publication Date: 2012-06-20
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] To sum up, the existing crystal form of agomelatine has high production cost and cumbersome operation, and the water solubility of the existing crystal form of agomelatine is not good, which affects the efficacy of the medicine. Therefore, it is necessary to prepare a water-soluble Agomelatine crystal form with good properties and simple preparation method

Method used

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  • Agomelatine-isonicotine eutectic crystal and compound and preparation method thereof
  • Agomelatine-isonicotine eutectic crystal and compound and preparation method thereof
  • Agomelatine-isonicotine eutectic crystal and compound and preparation method thereof

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preparation example Construction

[0042] The preparation method of agomelatine-isonicotine co-crystal comprises the steps:

[0043] 1) Mix agomelatine and isonicotine at a molar ratio of 1:1;

[0044] 2) heating the mixture to melt;

[0045] 3) cooling and washing to obtain agomelatine-isonicotine co-crystal.

[0046] The melting temperature should ensure that both agomelatine and isonicotine are completely melted and not decomposed, and the melted compounds can be uniformly mixed at the molecular level. Considering actual production, the melting temperature can be selected to be 120-150°C, preferably 125-140°C.

[0047] Preferably, in order to ensure that the compounds are mixed uniformly and the prepared eutectic has high purity, the temperature is kept constant for not less than 30 minutes after melting. In order to ensure that it mixes evenly, it can be stirred properly when melting.

[0048] Preferably, after cooling, the obtained solid is washed twice with water.

Embodiment 1

[0051] Mix 50mg agomelatine and 25mg isonicotine evenly, seal it, heat it to 130°C for 1 hour, then cool it down to room temperature naturally, wash the obtained white solid twice with 5mL water, and dry to obtain 73.5mg of white solid, the yield 98%, melting point 119-121°C.

Embodiment 2

[0053]Mix 100mg agomelatine and 50mg isonicotine evenly, seal, heat to 128°C, after 1h, cool down to room temperature naturally, wash the obtained white solid twice with 10mL water, dry to obtain 145.5g white solid, yield 97%, melting point 119-121°C. The resulting solid was dissolved in tetrahydrofuran, filtered, and the filtrate was left to evaporate to obtain colorless blocky crystals.

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Abstract

The invention discloses agomelatine-isonicotine eutectic crystal which has the chemical formula (I). The diffraction angles 2theta can be 10.20 DEG, 14.43 DEG, 15.97 DEG, 17.64 DEG, 18.57 DEG, 19.22 DEG, 19.91 DEG, 20.68 DEG, 21.39 DEG, 21.66 DEG, 21.94 DEG, 23.16 DEG, 24.28 DEG, 24.75 DEG, 25.42 DEG, 29.54 DEG, 29.90 DEG and 30.39 DEG. The agomelatine-isonicotine eutectic crystal is prepared by melting agomelatine and isonicotine and cooling. The agomelatine-isonicotine eutectic crystal is easy to prepare and has low preparation cost.

Description

technical field [0001] The invention relates to an agomelatine-isonicotine co-crystal, a composition and a preparation method thereof. Background technique [0002] Agomelatine (agomelatine), the chemical name is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, and its structural formula is: [0003] [0004] Agomelatine is a new antidepressant drug with a new mechanism of action. Its trade name is Valdoxan. It is the first melatonin antidepressant developed by the French company Servier. It can effectively treat depression and improve sleep. parameters, characteristics that do not affect sexual function. Agomelatine was synthesized and reported for the first time in 1992, and was approved for marketing in the European Union in February 2009. [0005] The listing of agomelatine is a new breakthrough in the field of depression treatment. It has two unique mechanisms of action. First, agomelatine is melatonin (MT 1 MT 2 ) receptor agonist, MT 1 MT 2 Receptors are densely...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/81C07C233/18A61K31/4409A61K31/165A61P25/24
Inventor 闫岩鲁统部陈嘉媚
Owner SUN YAT SEN UNIV
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