A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/635 (2006.01) A61K 9/50 (2006.01) A61K 9/14 (2006.01) A61K 9/20 (2006.01)
Patent
CA 2595496
The invention relates to a medicament which is intended for oral administration, which comprises a cyclooxygenase-2 inhibitor and which has improved bioavailability, and to a method of preparing said medicament. The inventive medicament comprises an agglomerate based on inert solid particles based on at least one excipient, said agglomerate comprising a cyclooxygenase-2 inhibitor and at least one hydrophilic polymer. According to the invention, the agglomerate comprises a spray which is applied to the aforementioned particles, consisting of a solution or suspension of micronized grains of the inhibitor in said polymer(s), in order to agglomerate said particles. The inventive method essentially comprises the following steps, namely: (i) the preparation of a sprayable liquid that is based on the micronized grains of said inhibitor in solution or in suspension in at least one hydrophilic polymer; and (ii) the spraying of the liquid onto the solid particles, in order to obtain the agglomerate by means of wet granulation, said agglomerate comprising the grain solution or suspension spray.
La présente invention concerne un médicament destiné à être administré par voie orale qui comprend un inhibiteur de la cyclo-oxygénase-2 et qui présente une biodisponibilité améliorée, et un procédé de préparation de ce médicament. Un médicament selon l'invention comprend un agglomérat à base de particules solides inertes à base d'au moins un excipient, l'agglomérat comprenant un inhibiteur de la cyclo-oxygénase-2 et au moins un polymère hydrophile, et il est tel que cet agglomérat comprend le produit de pulvérisation sur ces particules d'une solution ou suspension de grains micronisés de cet inhibiteur dans ce(s) polymère(s), pour agglomérer ces particules. Un procédé selon l'invention comprend essentiellement : (i) la préparation d'un liquide pulvérisable à base de grains micronisés de cet inhibiteur en solution ou en suspension dans au moins un polymère hydrophile, (ii) une pulvérisation du liquide sur ces particules solides, pour l'obtention par granulation par voie humide de l'agglomérat comprenant le produit de pulvérisation de la dissolution ou suspension des grains.
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