Ph-sensitive polymer

Details Ph-sensitive polymer Ph-sensitive polymer

C - Chemistry, Metallurgy

08

F

C08F 220/12 (2006.01) A61K 47/32 (2006.01) A61K 47/48 (2006.01) C07H 21/00 (2006.01) C07K 17/08 (2006.01) C08F 220/06 (2006.01)

Patent

CA 2480273

The invention relates to a pH-sensitive polymer which is a (meth)acrylate copolymer composed of 20 to 65 % by weight acrylic and/or methacrylic acid units and 80 to 35 % by weight units of C1- to C18-alkyl esters of (meth)acrylic acid, characterized in that it has a molecular weight in the range from 1 000 to 50 000 g/mol, and brings about at least 60 % haemolysis at pH 5.5, and less than 5 % haemolysis at pH 7.4, in a concentration of 150 µg/ml in a cytotoxicity test with human red blood cells. The invention further relates to the use of the pH-sensitive polymer as carrier for pharmaceutically effective biomolecules or active pharmaceutical ingredients and as ingredient of corresponding dosage forms.

L'invention concerne un polymère sensible au pH, qui est un copolymère de (méth)acrylate renfermant, en poids, entre 20 et 65 % d'unités d'acide acrylique et/ou méthacrylique, et entre 80 et 35 % d'unités d'esters d'alkyle C¿1?-C¿18? d'acide (méth)acrylique, de poids moléculaire compris entre 1 000 et 50 000 g/mol, induisant au moins 60 % d'hémolyse à un pH de 5,5, et moins de 5 % d'hémolyse à un pH de 7,4, pour une concentration de 150 µg/ml, dans un test de cytotoxicité réalisé avec des globules rouges humains. L'invention concerne en outre l'utilisation de ce polymère comme vecteur de biomolécules pharmaceutiquement efficaces ou de principes pharmaceutiques actifs, et comme principe de formes pharmaceutiques correspondantes.

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