Self-emulsifying formulation for lipophilic compounds

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/107 (2006.01) A61K 9/48 (2006.01) A61K 31/20 (2006.01) A61K 31/23 (2006.01) A61K 31/4433 (2006.01)

Patent

CA 2294031

The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di-unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

La présente invention concerne une nouvelle composition pharmaceutique basée sur l'utilisation d'une phase huileuse, cette composition renfermant: un agent lipophile pharmaceutiquement actif; un mélange de diglycéride et de monoglycéride présentant un rapport variant environ entre 9:1 et 6:4 en poids (diglycéride:monoglycéride), le diglycéride et le monoglycéride étant des esters d'acides gras de glycérol mono-insaturés ou di-insaturés, de longueur de chaîne de seize à vingt-deux atomes de carbone; un ou plusieurs solvants pharmaceutiquement acceptables; et un ou plusieurs tensioactifs pharmaceutiquement acceptables. Cette composition se présente sous la forme d'une formulation autoémulsifiante, présentant une concentration élevée en composés lipophiles et une biodisponibilité orale importante pour ces derniers.

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