Liposome microreservoir composition and method

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2067133

A liposome composition for extended release of a therapeutic compound into the bloodstream. The liposomes are composed of vesicle-forming lipids and between l-20 mole percent of a vesicle-forming lipid derivatized with hydrophilic polymer, have sizes in a selected size range between 0.1 and 0.4 microns, and contain the therapeutic compound in liposome-entrapped form. The dosage form of the composition contains at least about three times the dose of the compound required for intravenous injection in free form. Also disclosed is a method for extending to at least 24 hours the period in which an intravenously administered therapeutic compound is therapeutically active in the blood-stream, and novel liposomes for practicing the method.

Composition liposomique pour libération prolongée d'un composé thérapeutique dans la circulation sanguine. Les liposomes sont constitués de lipides formant des vésicules et de l à 20 % en moles d'un lipide formant des vésicules, avec dérivatisation par un polymère hydrophile; ils ont une taille comprise entre 0,1 et 0,4 micron et renferment le composé thérapeutique sous forme de piège liposomique. La forme posologique de la composition contient au moins trois fois la dose de composé requise pour l'injection veineuse sous forme libre. L'invention présente également une méthode pour étendre à au moins 24 heures la période pendant laquelle un composé thérapeutique administré par voie veineuse est actif dans la circulation sanguine, ainsi que de nouveaux liposomes pour appliquer la méthode.

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