Method for loading lipid vesicles

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/127 (2006.01) A61K 31/47 (2006.01) A61K 31/475 (2006.01) A61K 31/495 (2006.01) A61K 31/71 (1995.01)

Patent

CA 2213861

Methods for the preparation of stable liposome formulations of protonatable therapeutic agents. The methods involve loading a therapeutic agent into preformed liposomes having a methylamine concentration gradient across the lipid bilayer of the liposomes. These methods provide liposome formulations which are more stable, more cost effective, and easier to prepare in a clinical environment than those previously available. The present invention also provides the pharmaceutical compositions prepared by the above methods, a kit for the preparation of liposome formulations of therapeutic agents, and methods for their use.

La présente invention concerne des procédés de préparation de formulations stables de liposomes d'agents thérapeutiques pouvant subir une protonation. Ces procédés comprennent le chargement d'un agent thérapeutique dans des liposomes formés à l'avance et présentant un gradient de concentration en méthylamine au travers de la double couche lipidique des liposomes. Ces procédés donnent des formulations de liposomes qui sont plus stables, plur rentables et plus faciles à préparer en milieu clinique que celles existant auparavant. La présente invention concerne aussi les compositions pharmaceutiques préparées suivant les procédés ci-dessus, un kit de préparation de formulations de liposomes d'agents thérapeutiques et des méthodes d'utilisation.

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