Chroman derivative containing ophthalmic solution

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/415 (2006.01) A61K 9/00 (2006.01) A61K 9/08 (2006.01) A61K 31/4178 (2006.01) A61K 47/38 (2006.01)

Patent

CA 2246224

The object of the present invention is to provide an ophthalmic solution with improvement in the ocular penetration of (2S, 4S)-6-fluoro-2',5'-dioxospiro[chroman-4,4'- imidazolidine]-2-carboxamide as an active ingredient. The ophthalmic solutior of the present invention comprises (2S, 4S)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2- carboxamide as an active ingredient whereln the osmotic pressure ratio is adjusted to less than 1 and the viscosity to more than 1 cP thereby ocular penetration of the active ingredient are remarkably improved. As a viscosity increasing agent, a cellulose-based polymer for example is formulated. The cellulose-based polymer is preferably hydroxypropylmethylcellulose.

La présente invention porte sur une solution ophtalmique à pénétration oculaire améliorée, à base de (2S, 4S)-6-fluoro-2',5'-dioxospiro¢chroman-4,4'- imidazolidine!-2-carboxamide comme ingrédient actif. Pour la solution ophtalmique de la présente invention, qui renferme du (2S, 4S)-6-fluoro-2',5'-dioxospiro¢chroman-4,4'-imidazolidine!-2- carboxamide comme ingrédient actif, le taux de pression osmotique est ajusté à moins de 1 et la viscosité à plus de 1 cP, ce qui améliore de façon remarquable la pénétration oculaire de l'ingrédient actif. Comme agent augmentant la viscosité, on donne par exemple une formulation de polymère à base de cellulose. Le polymère cellulosique est préférablement à base de l'hydroxypropylméthylcellulose.

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