Methods for the controlled delivery of pharmacologically...

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01)

Patent

CA 2535373

The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water immiscible solvent. In one embodiment the compositions are provided as injectable compositions. The lipophilic counterion may be a saturated or unsaturated C8- C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. The compositions are released over time when administered to a mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for periods of up to 15 days or even longer. Many compounds can be administered according to the present invention, including, but not limited to, tilmicosin, oxytetracycline, fluoxetine, roxithromycin, and turbinafine.

L'invention concerne des compositions et des procédés permettant de prolonger les temps de libération et de réduire la toxicité de composés pharmacologiquement actifs. Lesdits composés comprennent un sel du composé pharmacologiquement actif avec un contre-ion lipophile et un solvant non miscible avec l'eau pharmaceutiquement acceptable. Dans un mode de réalisation, ces compositions sont des compositions injectables. Le contre-ion lipophile peut être un acide gras C¿8?-C¿22? saturé ou insaturé, de préférence un acide gras C¿10?-C¿18? saturé ou insaturé. Les compositions sont libérées progressivement lorsqu'elles sont administrées à un mammifère. L'invention permet ainsi d'administrer des doses contrôlées de composé actif sur des périodes allant jusqu'à 15 jours ou plus. Divers composés peuvent être administrés selon l'invention, ces composés comprenant, de façon non limitative, la tilmicosine, l'oxytétracycline, la fluoxétine, la roxithromycine et la turbinafine.

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