OPHTHALMIC PHARMACEUTICAL COMPOSITION

20140018316

14/029332

September 17, 2013

The present invention has an object to provide an ophthalmic pharmaceutical composition, particularly, an ophthalmic solution, ophthalmic ointment, ophthalmic wash, intraocular infusion solution, wash for anterior chamber, internal medicine, injection, or preservative for extracted cornea, which has improved therapeutic and/or prophylactic effects on the swelling, edema and walleye/cloudiness in the lens and/or the cornea induced by ophthalmic diseases including cataract and which is safe and successively used for a relatively long period of time. The present invention solves the above object by providing an ophthalmic pharmaceutical composition incorporated with a saccharide having a basic structure consisting of four glucose molecules bound together in a cyclic manner via a specific binding fashion.

1. A method for treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea, which comprises a step of administering a composition to a subject's eye(s), said composition consisting of i) a saccharide having a basic structure represented by General Formula 1, ii) water, and iii) one or more members selected from the group consisting of maltose, sodium chloride, potassium chloride, sodium dihydrogenphosphate, calcium chloride, magnesium chloride, sodium citrate, sodium hydrogencarbonate, borax, D-glucose, benzalkonium chloride, α,α-trehalose, ascorbic acid 2-glucoside, hydrochloric acid, liquid paraffin, white petrolatum, physiological saline, and magnesium sulfate, wherein the content of said saccharide i) to the total saccharide content in said composition is 98% or higher, said composition being in the form of a member selected from the group consisting of ophthalmic solution, ophthalmic wash, ophthalmic ointment, and injection, wherein the amount of said saccharide i) in said composition is about 0.1 to 20% to the total weight of said composition, thereby treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea: [chemical expression included] where, R1 through R12 independently represent a substituent selected from the group consisting of hydroxyl group, O-glycosyl group, and O-alkyl group.

2. The method of claim 1, wherein said saccharide having a basic structure represented by General Formula 1 is a cyclic tetrasaccharide having a cyclic structure of cyclo{→6)-α-D-glucopyranosyl-(1→3)-α-D-glucopyranosyl-(1→6)-α-D-glucopyranosyl-(1→3)-α-D-glucopyranosyl-(1→}.

3. The method of claim 1, wherein the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea are induced by cataract.

4. A method for treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea, which comprises a step of administering a composition to a subject's eye(s), said composition consisting of i) a saccharide having a basic structure represented by General Formula 1, ii) water, and iii) one or more members selected from the group consisting of maltose, sodium chloride, potassium chloride, sodium dihydrogenphosphate, calcium chloride, magnesium chloride, sodium citrate, sodium hydrogencarbonate, borax, D-glucose, benzalkonium chloride, α,α-trehalose, ascorbic acid 2-glucoside, hydrochloric acid, liquid paraffin, white petrolatum, physiological saline, and magnesium sulfate, wherein the content of said saccharide i) to the total saccharide content in said composition is 98% or higher, said composition being in the form of a member selected from the group consisting of ophthalmic solution, ophthalmic wash, ophthalmic ointment, and injection, wherein the amount of said saccharide i) in said composition is at least 0.01% by weight to the total weight of said composition, thereby treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea: [chemical expression included] where, R1 through R12 independently represent a substituent selected from the group consisting of hydroxyl group, O-glycosyl group, and O-alkyl group.

5. A method for treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea, which comprises a step of administering a composition to a subject's eye(s), said composition consisting of i) a saccharide having a basic structure represented by General Formula 1, ii) water, and iii) one or more members selected from the group consisting of maltose, sodium chloride, potassium chloride, sodium dihydrogenphosphate, calcium chloride, magnesium chloride, sodium citrate, sodium hydrogencarbonate, borax, D-glucose, benzalkonium chloride, α,α-trehalose, ascorbic acid 2-glucoside, hydrochloric acid, liquid paraffin, white petrolatum, physiological saline, and magnesium sulfate, wherein the content of said saccharide i) to the total saccharide content in the composition is 98% or higher; iv) and at least one optional ingredients selected from the group consisting of alcohols, p-oxymethyl benzoate, sodium dehydroacetate, buffers, thickeners, solubilizing agents, stabilizers, bases for ophthalmological ointment, and mixtures thereof, said composition being in the form of a member selected from the group consisting of ophthalmic solution, ophthalmic wash, ophthalmic ointment, and injection; and wherein the amount of said saccharide i) in said composition is about 0.1 to 20% to the total weight of said composition, thereby treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea: [chemical expression included] where, R1 through R12 independently represent a substituent selected from the group consisting of hydroxyl group, O-glycosyl group, and O-alkyl group.

6. The method according to claim 5, wherein the buffer is boric acid; the thickeners are selected from the group consisting of methyl cellulose, carboxymethyl cellulose, chondroitin sulfate, polyvinyl alcohol, and pullulan; the stabilizing agents are polysorbate 80; and the stabilizers are selected from the group consisting of sodium edetate and sodium hydrogensulfite.

7. A method for treating the swelling, edema and/or walleye/cloudiness of the lens and/or the cornea, which comprises a step of administering a composition to a subject's eye(s), said composition consisting of: i) a saccharide having a basic structure represented by General Formula 1, ii) water; and iii) one or more members selected from the group consisting of maltose, sodium chloride, potassium chloride, sodium dihydrogenphosphate, calcium chloride, magnesium chloride, sodium citrate, sodium hydrogencarbonate, borax, D-glucose, sterile refined water, benzalkonium chloride, α,α-trehalose, ascorbic acid 2-glucoside, hydrochloric acid, liquid paraffin, white petrolatum, physiological saline, and magnesium sulfate, wherein the content of said saccharide i) to the total saccharide content in said composition is 98% or higher, said composition being in the form of a member selected from the group consisting of intraocular infusion solution, wash for anterior chamber, internal medicine, or preservative for extracted cornea; and wherein the amount of said saccharide i) in said composition is about 0.1 to 20% to the total weight of said composition, thereby treating the swelling, edema and/or walleye/cloudiness in the lens and/or the cornea: [chemical expression included] where, R1 through R12 independently represent a substituent selected from the group consisting of hydroxyl group, O-glycosyl group, and O-alkyl group.

514/61

61; 61

edspap.20140018316