Ophthalmic compositions containing a synergistic combination of two polymers

• US 20040253280A1
• Filed: 06/08/2004
• Published: 12/16/2004
• Est. Priority Date: 06/13/2003
• Status: Active Grant

• Current Assignee: Novartis Ag
• Original Assignee: Alcon Incorporated
• Inventors: Chowhan, Masood A., Chen, Huagang
• Granted Patent: US 7,709,012 B2
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/04 Artificial tears; Irrigation solutions
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

Ophthalmic compositions suitable for use as artificial tears or as vehicles for ophthalmic drugs are disclosed. The compositions contain a combination of two polymers that have a synergistic effect on viscosity.

Claims

1. An aqueous composition suitable for topical ophthalmic administration comprising a viscosity enhancing amount of combination of two polymers having a synergistic effect on the composition'"'"'s viscosity and wherein the combination of two polymers is selected from the group consisting of hydroxypropyl methylcellulose and guar gum;

hydroxypropyl methylcellulose and a carboxyvinyl polymer;

a carboxyvinyl polymer and guar gum;

hydroxypropyl methylcellulose and hydroxyethylcellulose;

hyaluronic acid and hydroxypropyl methylcellulose; and

hyaluronic acid and guar gum, provided that if the composition comprises a carboxyvinyl polymer then the composition does not contain sodium chloride or boric acid.

2. The composition of claim 1 wherein the combination of two polymers is a combination of a hydroxypropyl methylcellulose and guar gum.

3. The composition of claim 1 wherein the combination of two polymers is a combination of hydroxypropyl methylcellulose and a carboxyvinyl polymer.

4. The composition of claim 1 wherein the combination of two polymers is a combination of a carboxyvinyl polymer and guar gum.

5. The composition of claim 1 wherein the combination of two polymers is a combination of hydroxypropyl methylcellulose and hydroxyethylcellulose.

6. The composition of claim 1 wherein the combination of two polymers is a combination of hyaluronic acid and hydroxypropyl methylcellulose.

7. The composition of claim 1 wherein the combination of two polymers is a combination of hyaluronic acid and guar gum.

8. The composition of claim 1 wherein the carboxyvinyl polymer is a polymer of acrylic acid crosslinked with allyl sucrose or allylpentaerythritol, the hydroxypropyl methylcellulose has a number average molecular weight of approximately 86,000 dalton, the guar gum is hydroxypropyl guar.

9. The composition of claim 1 wherein the total concentration of the two polymers ranges from 0.05-3.0% (w/w).

10. The composition of claim 9 wherein the total concentration of the two polymers ranges from 0.2-2.0% (w/w).

11. The composition of claim 1 further comprising an ingredient selected from the group consisting of pharmaceutically acceptable buffering agents;

preservatives;

non-ionic tonicity-adjusting agents;

surfactants;

solubilizing agents;

stabilizing agents;

comfort-enhancing agents;

emollients;

pH-adjusting agents; and

lubricants.

12. The composition of claim 1 further comprising an ophthalmic drug.

13. The composition of claim 12 wherein the ophthalmic drug is selected from the group consisting of anti-glaucoma agents;

anti-angiogenesis agents;

anti-infective agents;

non-steroidal and steroidal anti-inflammatory agents;

growth factors;

immunosuppressant agents; and

anti-allergic agents.

14. A method of alleviating the symptoms of dry eye comprising topically administering to the eye an aqueous composition comprising a viscosity enhancing amount of a combination of two polymers having a synergistic effect on the composition'"'"'s viscosity and wherein the combination of two polymers is selected from the group consisting of hydroxypropyl methylcellulose and guar gum;

hydroxypropyl methylcellulose and a carboxyvinyl polymer;

a carboxyvinyl polymer and guar gum;

hydroxypropyl methylcellulose and hydroxyethylcellulose;

hyaluronic acid and hydroxypropyl methylcellulose; and

hyaluronic acid and guar gum, provided that if the composition comprises a carboxyvinyl polymer then the composition does not contain sodium chloride or boric acid.