Amplification of the vitamin b12 uptake system using polymers

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01) A61K 38/09 (2006.01) C07K 7/02 (2006.01) C07K 7/23 (2006.01) C07K 14/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2163226

The invention relates to the oral delivery of peptide and protein pharmaceuticals using the vitamin B12 (VB12) uptake system, with the delivery being amplified using polymers. More particularly, the invention concerns a complex having the general formula: (V - Q)n - P - (Q' - A)m where, V is a carrier which will bind to natural intrinsic factor (IF) selected from vitamin B12 or an analogue thereof, n is the molar substitution ratio of V in the complex, and is a number from 1.0 to about 10, P is a pharmaceutically acceptable polymer, A is a pharmaceutically active substance, m is the molar substitution ratio of A in the complex, and is a number greater than 1.0 to about 1000, Q and Q' are independently a covalent bond, or a spacer compound linking V, P and A by covalent bonds.

L'invention concerne la diffusion par voie orale de produits pharmaceutiques à base de peptides et de protéines grâce à l'utilisation du système d'absorption de la vitamine B12, cette diffusion étant amplifiée par des polymères. L'invention concerne plus particulièrement un complexe de formule générale: (V - Q)n - P - (Q - A)m, où V représente un vecteur qui se lie à un facteur intrinsèque naturel choisi entre la vitamine B12 ou l'un de ses analogues, n représente le rapport de substitution molaire de V dans ce complexe, rapport compris entre 1 et environ 10, P représente un polymère pharmaceutiquement acceptable, A représente une substance pharmaceutiquement active, m représente le rapport de substitution molaire de A dans ce complexe, rapport compris entre 1 et environ 1000, et Q et Q' représentent indépendamment une liaison covalente ou un composé d'écartement reliant V, P et A par des liaisons covalentes.

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