Granulation of active pharmaceutical ingredients

A - Human Necessities – 61 – K

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Details

A61K 9/16 (2006.01) A61K 9/20 (2006.01)

Patent

CA 2720744

The present invention discloses a dry formulation or granulation comprising, in admixture, more than 50 wt.% of active pharmaceutical ingredient and from 1 to 10 wt.% of each of any nonaqueous excipient selected from liquid substances. In a preferred embodiment no water or lower alcohol has been added in any step of the preparation of the dry formulation or granulation, and the nonaqueous excipient selected from liquid substances is adsorbed to dryness by the active pharmaceutical ingredient and/or by a further solid excipient. Pharmaceutical formulations based on such dry formulation or granulation, and processes for the preparation thereof, are described as well. The dry formulations or granulations reliably and effectively further processed under dry conditions without requiring active drying, including e.g. briquetting, slugging, sieving, milling, tabletting, further fine granulating, direct compression, and the like.

La présente invention concerne une formulation ou granulation sèche comprenant, en mélange, plus de 50 % en poids de composant pharmaceutique actif et de 1 à 10 % en poids de tel ou tel excipient non aqueux choisi parmi des substances liquides. Dans un mode de réalisation préféré, il n'est ajouté d'eau ou d'alcool inférieur dans aucune étape de la préparation de la formulation ou granulation sèche et lexcipient non aqueux choisi parmi des substances liquides est adsorbé à sec par le composant pharmaceutique actif et/ou par un autre excipient solide. Des formulations pharmaceutiques basées sur une telle formulation ou granulation sèche, et des procédés pour la préparation de celles-ci, sont également décrits. Les formulations ou granulations sèches peuvent être traitées plus avant de manière fiable et efficace dans des conditions sèches sans nécessiter un séchage actif, par exemple par briquetage, par pistonnage, par tamisage, par broyage, par compression, granulation fine supplémentaire, compression directe, et autres opérations similaires.

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