Drug delivery system based on regioselectively amidated...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2658587

New drug delivery systems (DDS) are described containing hyaluronic acid and a therapeutic agent, wherein the therapeutic agent is linked, directly or via a linker, to 6-aminohyaluronic acid and where the linkage of the drug or linker with 6-aminohyaluronic acid is realised by an amide bond. Preferred therapeutic agents for use in the present DDS are anti-inflammatory, antibiotic, antitumor drugs. Preferred linkers are: succinic acid, succinic acid linked to aminoacids, succinic acid linked to peptides. The DDS are stable and free of undesired reaction by-products and impurities, and show a high level of pharmacological efficacy.

La présente invention concerne de nouveaux systèmes d'administration de médicaments contenant de l'acide hyaluronique et un agent thérapeutique, ledit agent thérapeutique étant lié, directement ou via un lieur, à l'acide 6-aminohyaluronique et la liaison du médicament ou du lieur avec l'acide 6-aminohyaluronique étant réalisée par une liaison amide. Des agents thérapeutiques préférés pour une utilisation dans les systèmes d'administration de médicaments selon la présente invention sont: des médicaments anti-inflammatoires, antibiotiques, anti-tumoraux. Des lieurs préférés sont: l'acide succinique, l'acide succinique lié à des acides aminés, l'acide succinique lié à des peptides. Les systèmes d'administration de médicaments sont stables et exempts sous-produits et d'impuretés à réaction indésirable, et présentent un niveau élevé d'efficacité pharmacologique.

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