Pharmaceutical solid preparation comprising benzazepines and...

A - Human Necessities – 61 – K

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A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 9/26 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2689467

The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50 wt.% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70µm, and a 90% cumulative particle diameter of 100 to 200µm.

L'invention concerne une nouvelle préparation solide pharmaceutique qui présente des propriétés supérieures de désintégration et une excellente solubilité permettant d'assurer un pouvoir d'absorption suffisant de principes actifs par le système gastro-intestinal. La préparation solide pharmaceutique de l'invention comprend : (a) du 7-chloro-5-hydroxy-1-[2-méthyl-4-(2-méthylbenzoylamino)benzoyl]-2,3,4,5-tétrahydro-1H-benzoazépine et/ou un sel de celui-ci; (b) de l'hydroxypropylcellulose contenant un groupe hydroxypropoxyle à une quantité supérieure ou égale à 50 % en poids; et (c) au moins un élément sélectionné dans le groupe comprenant carmellose, sodium carboxyméthyl amidon, crospovidone, et hydroxypropylcellulose faiblement substituée présentant un diamètre moyen de particules compris entre 30 et 70 µm, et un diamètre cumulé de particules de 90% compris entre 100 et 200 µm.

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