Pharmaceutical compositions for oral administration

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01)

Patent

CA 2396379

The invention relates to the use of multilamellar vesicles which comprise a lamellar liquid crystal internal structure made up of amphiphilic agent-based concentric bylayers alternated with layers of water, aqueous solution or a solution of a polar liquid; from the center to the periphery of the vesicles, and in which at least one active agent is incorporated, for producing an orally administered pharmaceutical composition. Said vesicles act as vectors of the active agent and enable said active agent to cross the gastro- intestinal barrier more easily. The vesicles also protect the active agent from decomposition, especially decomposition by the enzymes present in the gastro-intestinal environment. The invention also relates to novel compositions for oral administration, especially compositions containing heparin, incorporated in vesicles such as those described above.

L'invention concerne l'utilisation de vésicules multilamellaires présentant une structure interne cristal-liquide lamellaire formée d'un empilement de bicouches concentriques à base d'agents amphiphiles alternant avec des couches d'eau, de solution aqueuse ou de solution d'un liquide polaire et au sein desquelles se trouve incorporé au moins un principe actif, pour la fabrication d'une composition pharmaceutique destinée à une administration par voie orale. Ces vésicules jouent le rôle de vecteurs du principe actif et facilitent son passage à travers la barrière gastro-intestinale. Elles permettent également de le protéger de la dégradation, en particulier de la dégradation par les enzymes présentes dans le milieu gastro-intestinal. L'invention concerne également de nouvelles compositions destinées à être administrées par voie orale, en particulier des compositions contenant de l'héparine incorporée dans des vésicules telles que définies ci-dessus.

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