OPHTHALMIC COMPOSITIONS CONTAINING A SYNERGISTIC COMBINATION OF THREE POLYMERS

• US 20080193407A1
• Filed: 02/08/2008
• Published: 08/14/2008
• Est. Priority Date: 02/09/2007
• Status: Abandoned Application

• Current Assignee: Novartis Ag
• Original Assignee: Alcon Incorporated
• Inventors: Chowhan, Masood A., Chen, Huagang
• Application Number:
  US12/028,111
• Publication Number:
  US 20080193407A1
• Time in Patent Office: Days
• US Class Current: 424/78.04
• CPC Class Codes: A61K 31/74 Synthetic polymeric materials
• 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 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics

Abstract

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

Claims

1. An aqueous composition suitable for ophthalmic administration comprising three polymeric ingredients having a synergistic effect on the composition'"'"'s viscosity wherein the three polymeric ingredients are a) hyaluronic acid, b) guar gum, and c) hydroxypropyl methylcellulose or a carboxyvinyl polymer, 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 hyaluronic acid ingredient is sodium hyaluronate and the guar gum ingredient is hydroxypropyl guar.

3. The composition of claim 1 wherein the composition comprises a carboxyvinyl polymer and the carboxyvinyl polymer is a polymer of acrylic acid crosslinked with allyl sucrose or allylpentaerythritol.

4. The composition of claim 1 wherein the three polymeric ingredients are present in a ratio of 1:

1;

1 to 3;

3;

3, and the total concentration of the three polymeric ingredients ranges from 0.1-1% (w/v).

5. The composition of claim 4 wherein the total concentration of the three polymeric ingredients ranges from 0.3-0.9% (w/v).

6. The composition of claim 5 wherein the total concentration of the three polymeric ingredients ranges from 0.3-0.7% (w/v).

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

preservatives;

tonicity-adjusting agents;

surfactants;

solubilizing agents;

stabilizing agents;

comfort-enhancing agents;

emollients;

pH-adjusting agents; and

lubricants.

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

9. The composition of claim 9 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.

10. An aqueous composition for use as an artificial tear wherein the composition consists essentially of a) hyaluronic acid;

b) hydroxypropyl guar;

c) hydroxypropyl methylcellulose or a carboxyvinyl polymer; and

d) mannitol, wherein the composition has a pH of 6-8 and an osmolality in the range of 220-340 mOsm/kg.

11. A method of alleviating the symptoms of dry eye comprising topically administering to the eye a composition comprising three polymeric ingredients having a synergistic effect on the composition'"'"'s viscosity wherein the three polymeric ingredients are a) hyaluronic acid, b) guar gum, and c) hydroxypropyl methyl cellulose or a carboxyvinyl polymer, provided that if the composition comprises a carboxyvinyl polymer then the composition does not contain sodium chloride or boric acid.

12. The method of claim 11 wherein the hyaluronic acid ingredient is sodium hyaluronate and the guar gum ingredient is hydroxypropyl guar.

13. The method of claim 11 wherein the composition comprises a carboxyvinyl polymer and the carboxyvinyl polymer is a polymer of acrylic acid crosslinked with allyl sucrose or allylpentaerythritol.

14. The method of claim 11 wherein the three polymeric ingredients are present in a ratio of 1:

1;

1 to 3;

3;

3, and the total concentration of the three polymeric ingredients ranges from 0.1-1% (w/v).

15. The method of claim 14 wherein the total concentration of the three polymeric ingredients ranges from 0.3-0.9% (w/v).

16. The method of claim 11 wherein the composition consists essentially of hyaluronic acid;

hydroxypropyl guar;

either hydroxypropyl methylcellulose or a carboxyvinyl polymer; and

mannitol, wherein the composition has a pH of 6-8 and an osmolality in the range of 235-300 mOsm/kg.

17. A method of treating a disease or condition of the eye comprising administering to the eye a composition comprising an ophthalmic drug and a carrier wherein the carrier comprises three polymeric ingredients having a synergistic effect on the composition'"'"'s viscosity and wherein the three polymeric ingredients are a) hyaluronic acid, b) guar gum, and c) hydroxypropyl methyl cellulose or a carboxyvinyl polymer, provided that if the composition comprises a carboxyvinyl polymer then the composition does not contain sodium chloride or boric acid.

18. The method of claim 17 wherein the composition is administered topically to the eye.

19. The method of claim 17 wherein the composition is injected.

20. The method of claim 19 wherein the composition is injected as an intravitreal injection, subconjunctival injection, sub-tenon injection, retrobulbar injection, suprachoroidal injection, or periocular injection.

21. The method of claim 17 wherein the three polymeric ingredients are present in a ratio of 1:

1;

1 to 3;

3;

3, and the total concentration of the three polymeric ingredients ranges from 0.1-1% (w/v).