Topical ophthalmic preparations containing immunosuppressive...

A - Human Necessities – 61 – K

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Details

A61K 47/18 (2006.01) A61K 9/00 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2317010

Therapeutic preparations for topical ophthalmic application, containing from 0.02 to 5.0 weight % of immunosuppressive agents belonging to the groups of monocyclic undecapeptides, macrolide lactones or corticosteroids, in a vehicle comprising up to 10 weight % of polyalkyleneglycol-polyurethane copolymers. Said copolymers consist preferably of poly(oxy-1,2-ethanediyl)-.alpha.-hydro- .omega.-hydroxypolymers with 1,1'-methylene-bis-(4-isocyanatocyclohexane) having an average molecular weight of from 1000 to 3000 in a hydrophilic vehicle and preferably of poly[oxy(methyl-1,2-ethanediyl)]-.alpha.-hydro- .omega.-hydroxypolymers with 1,1'-methylene-bis-(4-isocyanatocyclohexane) having an average molecular weight of from 1600 to 18000 in a lipophilic vehicle. Said therapeutic agents can further contain additional excipients common in topical administration forms.

L'invention se rapporte à des préparations thérapeutiques conçues pour l'application ophtalmique topique, qui contiennent de 0,02 à 5 % en poids d'agents immunosuppresseurs appartenant aux groupes des undécapeptides monocycliques, des lactones macrolides et des corticostéroïdes, dans un excipient comportant jusqu'à 10 % en poids de copolymères de polyalkylèneglycol-polyuréthane. Lesdits copolymères sont constitués de préférence de poly(oxy-1,2-éthanediyl)-.alpha.-hydro-.omega.-hydroxypolymères associés à du 1,1'-méthylène-bis-(4-isocyanatocyclohexane) de poids moléculaire moyen compris entre 1000 et 3000 dans un excipient hydrophile et de préférence de poly(oxy-1,2-méthyl)-.alpha.-hydro-.omega.-hydroxypolymères associés à du 1,1'-méthylène-bis-(4-isocyanatocyclohexane) de poids moléculaire moyen compris entre 1600 et 18000 dans un excipient lipophile. Lesdits agents thérapeutiques peuvent également contenir des excipients supplémentaires habituellement utilisés dans les formulations pour application topique.

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