# US 5,710,182 A · Ophthalmic composition > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 5,710,182 A - Document ID: US5710182A - Status: Granted - Kind: A - Application number: 08/535,037 - Filed: 1996-04-02 - Granted: 1998-01-20 - Earliest claimed: 1994-03-31 - Assignees: Santen SAS - Inventors: Timo Reunamaki; Kari Lehmussaari; Eija Vartiainen; Olli Oksala; Sakari Alaranta - Web page: https://patentgrep.com/patent/US5710182A ## CPC - A61K 9/0048: {Eye, e.g. artificial tears} - A61P 27/02: Ophthalmic agents - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially of an ophthalmologically active agent, an ion sensitive, hydrophilic polymer in an amount a of 0.004 to 1.5% by weight, at least one salt selected from the group of inor ganic salts and buffers in a total amount of from 0.01 to 2.0% by weight, a wetting agent in an amount of 0 to 3.0% by weight, a preservative in an amount of 0 to 0.02% by weight, water, and optionally a pH regulating agent in an amount sufficient to give a pH of 4.0 to 8.0 to the composition, the ratio between salt and polymer components being such that the solution exhibits a viscosity of less than 1000 mPas. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics. ## Claims ### Claim 1 Ophthalmic composition in the form of a topical aqueous solution consisting essentially of an opthalmologically active agent, an ion sensitive, hydrophilic polymer in an amount of 0.004 to 1.5% by weight, at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0% by weight, a wetting agent in an amount of 0 to 3.0% by weight, a preservative in an mount of 0 to 0.02% by weight, water, and where the composition has a pH outside the range of 4.0 to 8.0, a pH regulating agent in an amount sufficient to give a pH of about 4.0 to about 8.0 to the composition, the ratio between salt and polymer being such that the solution exhibits a viscosity of less than 1000 centipoise. ### Claim 2 (depends on 1) The composition of claim 1, wherein the polymer is present in an amount of from 0.01 to 0.8% by weight and is selected from the group consisting of carbopol 907, 910, 934, 934P, 940, 941, 971, 971P, 974, 074P, 980 and 981. ### Claim 3 (depends on 1) The composition of claim 1 wherein the wetting agent is glycerol. ### Claim 4 (depends on 3) The composition of claim 3, wherein the amount of glycerol is 0.5 to 2.5% by weight. ### Claim 5 (depends on 1, 2) The composition of claim 1 or 2, wherein the salt is selected from the group consisting of sodium chloride, potassium chloride, sodium phosphates, sodium borate, sodium acetate, sodium citrate, equivalents and mixtures thereof. ### Claim 6 (depends on 1, 2) The composition of claim 1 or 2, wherein the viscosity is less than about 800 centipoise. ### Claim 7 (depends on 1, 2) The composition of claim 1 or 2, having a pH of 5.0 to 8.0. ### Claim 8 (depends on 1, 2) The composition of claim 1 or 2, wherein the ophthalmologically active agent is selected from the group consisting of antiglaucoma agents, sympathomimetic agents, sympatholytic agents, .beta.-blockers, carbonic anhydrase inhibitors, antibiotics, antiinflammatoric agents, antiallergic agents and mixtures thereof. ### Claim 9 (depends on 8) The composition of claim 8, wherein the pharmaceutically active agent is selected from the group consisting of betaxolol, carteolol, levobunolol, metipranolol, pindolol, propranolol and timolol, pilocarpine and mixtures thereof. ### Claim 10 (depends on 1) The composition of claim 1, consisting essentially of timolol in the form it its maleate salt or its hemihydrate in an amount of 0.1 to 0.5% by weight, calculated as the free base, polyacrylic acid in an amount of 0.04 to 0.4% by weight glycerol in an amount of 0.5 to 2.5% by weight sodium phosphates in an amount of 0.01 to 1.5% by weight, a preservative in an amount of 0 to 0.02% water, and, where the composition has a pH outside the range of 6.5 to 8, a pH-regulating agent in an amount sufficient to provide a pH of 6.5 to 8 of the composition wherein the viscosity of the solution is less than about 800 centipoise. ### Claim 11 (depends on 10) The composition of claim 10, the pH-regulating agent being selected from the group consisting of organic and inorganic bases and acids. ### Claim 12 (depends on 11) The composition of claim 11, wherein the pH-regulating agent is sodium hydroxide.