Method for utilizing neutral lipids to modify in vivo...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 9/107 (2006.01) A61K 47/44 (2006.01) G01N 33/92 (2006.01)

Patent

CA 2564120

The rate of release of encapsulated active compound from a multivesicular liposomal (MVL) formulation is modified by selection of a neutral lipid component. A family of MVL formulations containing different slow:fast release neutral lipid molar ratios displays different release rates depending upon the molar ratio of the fast release neutral lipid to the slow release neutral lipid in each member. Incubation in plasma or a plasma-like medium at in vivo temperatures so as to obtain a release rate curve for each allows selection from among the members of the family of a liposomal formulation with a desired rate of release in vivo.

La vitesse de libération d'un composé actif encapsulé depuis une formulation de liposomes multivésiculaires (LMV) est modifiée si le constituant est un lipide neutre. Des formulations de LMV contenant différents rapports molaires de lipides neutres à libération lente sur rapide présentent différentes vitesses de libération, selon le rapport molaire des lipides neutres à libération rapide par rapport aux lipides neutres à libération lente de chacune des formulations. Après une incubation dans le plasma ou dans un milieu apparenté au plasma aux températures in vivo afin d'obtenir une courbe de vitesse de libération pour chacune des formulations, il est possible de choisir parmi les formulations de liposomes celle qui présente la vitesse de libération désirée in vivo.

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