Oral pharmaceutical composition comprising an active...

A - Human Necessities – 61 – K

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A61K 9/107 (2006.01) A61K 9/48 (2006.01) A61K 31/366 (2006.01)

Patent

CA 2451855

The invention concerns an oral pharmaceutical composition designed to reduce the intestinal metabolism of the active principle it comprises, said composition being in the form of a self micro-emulsifying system in contact with an aqueous phase, comprising: a therapeutically efficient amount of said active principle; a lipophilic phase comprising a mixture of glycerol mono, di and triesters and PEG mono and diesters with at least a fatty acid selected in the group comprising C¿8?-C¿18? fatty acids; a surfactant phase comprising a mixture of glycerol mono, di and triesters and PEG mono and diesters with C¿8? caprylic acid and C¿10? capric acid; a cosurfactant phase comprising at least an alcohol ester with at least a fatty acid selected in the group comprising propylene glycol caprylic esters, propylene glycol lauric esters and polyglycerol oleic esters, the TA/CoTa ratio ranging between 0.2 and 6.

Utilisation d'une composition pharmaceutique ô usage oral pour diminuer le métabolisme intestinal du principe actif qu'elle contient, ladite composition se présentant sous forme d'un système auto-micro-émulsionable au contact d'une phase aqueuse, comprenant : - une quantité thérapeutiquement efficace dudit principe actif ;- une phase lipophile comprenant un mélange de mono, di, et triesters de glycérol et de mono et diesters de PEG avec au moins un acide gras choisi dans le groupe comprenant les acides gras en C8-C18 ;- une phase tensioactive comprenant un mélange de mono, di et triesters de glycérol et de mono et diesters de PEG avec les acides caprylique (C8) et caprique (C10) ; - une phase cotensioactive comprenant au moins un ester d'alcool avec au moins un acide gras choisi dans le groupe comprenant les esters caprylique du propylène glycol, les esters laurique du propylène glycol et les esters oléïque du polyglycérol.- le ratio TA/CoTA étant compris entre 0,2 et 6.

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