Crystalline base of escitalopram and orodispersible tablets...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 307/87 (2006.01)

Patent

CA 2612827

The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4- fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral- disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100 ~C, as well as a method for making such an orodispersible tablet.

L'invention porte: sur la base cristalline du médicament antidépresseur bien connu l'escitalopram, de formule S-1-[3-(diméthylamino)propyl]-1-(4-fluorophényl)-1,3-dihydro-5-isobenzofurancarbonitrile; sur un procédé de préparation de sels purifiés d'escitalopram, tels que l'oxalate, en utilisant la base; sur les sels obtenus au moyen dudit procédé; sur des préparations contenant lesdits sels; sur un procédé de préparation de base libre d'escitalopram ou de sels purifiés d'escitalopram, tels que l'oxalate, en utilisant l'hydrobromure; sur les sels obtenus au moyen dudit procédé; sur des préparations contenant lesdits sels; et finalement sur des comprimés orodispersibles d'une dureté de 22N et d'un temps de désintégration dans la bouche de moins de 120s, comportant un principe actif au point de fusion compris entre 40 et 100 °C, adsorbé sur une charge hydrosoluble, et sur un procédé d'obtention d'un tel comprimé.

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