Bioresponsive pharmacologically-active polymers and articles...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2243649

This invention relates to pharmacologically-active polymeric compounds; to substrates, such as implantable medical devices formed thereof or coated therewith; and to methods of using said compounds or said substrates for providing pharmacological agents released in response to in vivo activation at a desired location in a mammal. The polymeric material has a backbone comprising a pharmacologically-active fragment covalently linked through at least two functional groups within the backbone, wherein the backbone comprises, preferably, polyamide, polyurethane and/or polyurea linkages with, optionally, polyester, polycarbonate, polyether and/or polyvinyl linkages. The preferred pharmacological compounds are fluoroquinolines, particularly, ciprofloxacin. The pharmacologically-active compounds provide in vivo enhanced long-term anti-inflammatory, anti-bacterial, and-microbial and/or anti-fungal activity.

L'invention concerne: des composés polymères ayant un effet thérapeutique; des substrats, tels que des dispositifs médicaux implantables réalisés avec ces composés ou revêtus de ceux-ci; et des procédés pour utiliser ces composés ou ces substrats pour assurer une libération d'agents ayant un effet thérapeutique, suite à une activation in vivo, à un emplacement souhaité chez un mammifère. Le polymère a un squelette comprenant des groupes ayant un effet thérapeutique liés par covalence à au moins deux groupes fonctionnels dans le squelette, ce squelette contenant, de préférence, des liaisons polyamide, polyuréthane et/ou polyurée, avec, le cas échéant des liaisons polyester, polycarbonate, polyéther et/ou polyvinyle. Les composés à action pharmacologique préférés sont les fluoroquinolines, en particulier la ciprofloxacine. Les composés selon l'invention peuvent exercer in vivo une activité thérapeutique prolongée, par exemple anti-inflammatoire, antibactérienne, antimicrobienne et/ou antifongique.

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