Delivery of microparticle-conjugated drugs for inhibition of...

A - Human Necessities – 61 – K

Patent

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A61K 47/48 (2006.01) A61K 9/16 (2006.01) A61K 31/00 (2006.01) A61K 31/337 (2006.01) A61K 31/4353 (2006.01) A61K 49/00 (2006.01)

Patent

CA 2483456

Administration of a formulation comprising a antirestenotic compound conjugated to a microparticle carrier is effective to inhibit stenosis formation in a blood vessel. Such stenosis typically results, in the absence of treatment, from trauma to a vessel, such as an incision, excessive pressure, an angioplasty procedure and/or stent implantation. The antirestenotic compound is typically an antiproliferative, immunosuppressive, or anti-inflammatory drug, such as rapamycin, tacrolimus, paclitaxel, dexamethasone, or an active analog or derivative, an antisense oligonucleotide, or combinations thereof. The microparticle carrier comprises a suspension of gas-filled microbubbles or biocompatible polymeric microparticles, in a pharmaceutically acceptable liquid vehicle, and is effective to deliver the conjugated therapeutic to the site of vessel injury.

L'invention concerne l'administration d'une formulation comprenant un composé anti-resténose conjugué à un excipient micro-particulaire. Une telle administration est efficace pour inhiber une formation de sténose dans un vaisseau sanguin. Une telle sténose entraîne généralement, en l'absence de traitement, un traumatisme d'un vaisseau, tel qu'une incision, une pression excessive, une intervention d'angioplastie et/ou une implantation de stent. Le composé anti-resténose est généralement un médicament anti-prolifératif, immunosuppresseur ou anti-inflammatoire, tel que la rapamycine, le tacrolimus, le paclitaxel, la dexaméthasone, un analogue ou dérivé actif, un oligonucléotide antisens ou une combinaison de ces produits. L'excipient micro-particulaire comprend une suspension de micro-bulles remplies de gaz ou des micro-particules polymères biocompatibles, dans un véhicule liquide acceptable sur le plan pharmaceutique et il est efficace pour administrer l'agent thérapeutique conjugué dans le site de la blessure du vaisseau.

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