Liquid depot formulations

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/10 (2006.01) A61K 9/06 (2006.01) A61K 9/12 (2006.01)

Patent

CA 2569513

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non- parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Des pré-formulations comprenant des mélanges cristallins non liquides à faible viscosité contenant: a) au moins un lipide diacyle neutre et/ou au moins un tocophérol; b) au moins un phospholipide; c) au moins un solvant organique biocompatible contenant de l'oxygène et à faible viscosité, au moins un agent bioactif étant dissous ou dispersé dans le mélange à faible viscosité et les formes de la pré-formulation permettant la formation d'au moins une structure de phase cristalline liquide après contact avec un fluide aqueux. Les pré-formulations se prêtent à la préparation de compositions de dépôt topique et non parentéral ou parentéral en vue d'une libération prolongée d'agents actifs. Un procédé d'administration d'un agent actif consistant à administrer une pré-formulation, une méthode de traitement consistant à administrer une pré-formulation et l'utilisation de la pré-formulation dans un procédé de fabrication d'un médicament.

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