Liquid ophthalmic sustained release delivery system

Details Liquid ophthalmic sustained release delivery system Liquid ophthalmic sustained release delivery system

A - Human Necessities

61

K

A61K 47/36 (2006.01) A61K 9/00 (2006.01) A61K 9/08 (2006.01) A61P 27/02 (2006.01)

Patent

CA 2181715

Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is administrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05 % to about 10 % by weight of the polymer chitosan; said polymer consisting essentially of (A) monomeric .beta.(14)-D-glucosamine linked units and of (B) monomeric .beta.(14)-N-acetyl-D-glucosamine linked units which are scattered randomly in the molecule of the polymer, the numerical proportions of A and B being from about 60 to about 99 % of A and about 1 to about 40 % of B, the viscosity rating being from about 3 to about 3000 cps; in which method, upon contact with the higher pH of the ocular fluid, said liquid formulation is converted to a stiff gel from which the ophthalmic treating agent is slowly released over a prolonged period of time.

L'invention décrit un système de libération prolongée d'un liquide ophtalmique aqueux ainsi qu'un procédé pour effectuer une libération lente et prolongée d'agents de traitement ophtalmique dans les yeux d'un mannifère, ledit procédé consistant à administrer dans l'oeil dudit mammifère une quantité utile d'une composition pharmaceutique ophtalmique sous forme de liquide aqueux homogène, au pH compris entre environ 3,0 et environ 6,2, administrable sous forme de gouttes et renfermant une concentration ophtalmologiquement efficace d'un tel agent de traitement ophtalmique ainsi qu'environ 0,05 % à environ 10 % en poids du polymère chitosane, ledit polymère consistant essentiellement en: (A) des unités liées de .beta.(1?4)-D-glucosamine et en (B) des unités liées de .beta.(1?4)-N-acétyl-D-glucosamine monomères dispersées de façon aléatoire dans la molécule du polymère, les proportions numériques de A et B étant d'environ 60 % à environ 99 % de A et d'environ 1 % à environ 40 % de B, l'indice de viscosité étant d'environ 3 àenviron 3 000 cps; procédé selon lequel, au contact du pH plus élevé du liquide oculaire, ladite formulation liquide se transforme en un gel ferme d'où l'agent de traitement ophtalmique est lentement libéré pendant un laps de temps prolongé.

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