Solid-state form of celecoxib having enhanced bioavailability

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/12 (2006.01) A61K 9/14 (2006.01) A61K 9/20 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 45/06 (2006.01) A61P 29/00 (2006.01) C07D 213/61 (2006.01) C07D 261/08 (2006.01) C07D 307/58 (2006.01) C07D 311/58 (2006.01)

Patent

CA 2362673

The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.

Le celecoxib médicamenteux inhibant la cyclooxygénase-2 se présente sous une forme amorphe. L'invention porte également sur une substance médicamenteuse de celecoxib, dans laquelle le celecoxib est présent, au moins en quantité détectable, sous forme de celecoxib amorphe. L'invention concerne encore un composite inhibant la cristallisation du celecoxib, comprenant des particules de celecoxib amorphe ou une substance médicamenteuse à base de celecoxib intimement associée à un ou plusieurs inhibiteurs de cristallisation, par exemple des polymères. Elle concerne aussi une composition pharmaceutique comprenant ledit composition inhibant la cristallisation du celecoxib et un ou plusieurs principes actifs ainsi que des procédés de préparation de celecoxib amorphe, d'une substance médicamenteuse à base de celecoxib de l'invention, d'un composite inhibiteur de cristallisation de celecoxib de l'invention et d'une composition pharmaceutique de l'invention. Une méthode de traitement d'un état ou d'un trouble médical chez un sujet pour lequel un traitement à l'inhibiteur de cyclooxygénase-2 est indiqué, qui consiste à administrer, par exemple par voie orale, une composition de l'invention, en dose efficace au plan thérapeutique.

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