New crystalline form vi of agomelatine, preparation method...

C - Chemistry – Metallurgy – 07 – C

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C07C 233/18 (2006.01) A61K 31/165 (2006.01) A61P 1/00 (2006.01) A61P 5/00 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) A61P 25/18 (2006.01) A61P 25/20 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2754276

The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2.theta. 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.

La présente invention concerne une nouvelle forme cristalline de l'agomélatine, son procédé de préparation et son application. Dans le motif de diffraction des rayons X de la forme cristalline de la poudre d'agomélatine, on trouve des pics principaux où les angles de diffraction 2? valent 11,13, 11,82, 17,49, 18,29, 19,48, 19,72, 20,50, 21,76, 22,54, 22,97, 24,56, 25,36, 27,16 et 31,93. La nouvelle forme cristalline présente de bonnes pureté, stabilité et reproductibilité, et présente des avantages du point de vue pharmaceutique. De plus, ses stabilité et solubilité sont meilleures que celles des formes cristallines existantes.

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