Crystalline composition containing escitalopram oxalate

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 307/87 (2006.01) A61K 9/20 (2006.01) A61K 9/28 (2006.01) A61P 25/24 (2006.01) C07B 63/00 (2006.01) C07C 55/07 (2006.01)

Patent

CA 2558198

The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01 % (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl- benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate. Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

Cette invention concerne des particules cristallines d'oxalate d'escitalopram lesquelles présentent une répartition granulométrique étendue ou comprennent au moins 0,01 % (en poids) de Z-4-(4-diméthylamino-1-(4-fluorophényl)-but-1-enyl)-3-hydroxyméthyl-benzonitrile ; ces particules conviennent tout particulièrement à la compression directe. En outre, cette invention concerne une nouvelle forme posologique en dose unitaire de médicament contenant de telles particules cristallines d'oxalate d'escitalopram, ainsi que des procédés permettant de fabriquer ces particules cristallines d'oxalate d'escitalopram. Enfin, cette invention concerne également un procédé permettant de réduire la quantité d'impuretés contenant un hydroxyl dans une solution de citalopram ou d'escitalopram.

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