USE OF OCULOSURFACE SELECTIVE GLUCOCORTICOID IN THE TREATMENT OF DRY EYE

• US 20080096852A1
• Filed: 10/26/2007
• Published: 04/24/2008
• Est. Priority Date: 12/24/2002
• Status: Abandoned Application

• Current Assignee: Alcon Incorporated
• Original Assignee: Alcon Incorporated
• Inventors: Miller, Steven, YANNI, John, Gamache, Daniel, Castillo, Ernesto
• Application Number:
  US11/925,178
• Publication Number:
  US 20080096852A1
• Time in Patent Office: Days
• US Class Current: 514/179
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/186 Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
• 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 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/04 Artificial tears; Irrigation solutions

Abstract

Topical ophthalmic compositions and methods for treating dry eye are described. The compositions and methods of the invention are based on the finding that the oculosurface selective properties of the glucocorticoid rimexolone make this anti-inflammatory agent particularly well-suited for treating dry eye. As a result of the limited ability of rimexolone to penetrate the cornea, a high portion of the drug remains on the surface of the eye, which is the primary locus of the inflammatory conditions associated with dry eye. This enables a very low concentration of drug to be utilized, which in turn reduces the potential for elevations of intraocular pressure and cataract formation.

Claims

1. A method of treating chronic dry eye conditions, which comprises applying a therapeutically effective amount of a topical ophthalmic composition to the cornea of the affected eye on a daily basis for a period of from several weeks to several months or more, said composition comprising an effective amount of an oculosurface selective glucocorticoid.

2. A method according to claim 1, wherein the oculosurface selective glucocorticoid comprises rimexolone.

3. A method according to claim 2, wherein the composition contains rimexolone at a concentration of 0.001 to 0.1 w/v %.

4. A method according to claim 3, wherein the composition contains rimexolone at a concentration of less than 0.1 w/v %.

5. A method according to claim 4, wherein the composition contains rimexolone at a concentration of 0.05 to 0.075 w/v %.

6. A method according to claim 2, wherein the composition is a preserved, multi-dose composition.

7. A method according to claim 6, wherein the composition is an aqueous suspension, and further comprises an amount of polyvinyl pyrrolidone sufficient to suspend the rimexolone in the composition.

8. A method according to claim 7, wherein the composition further comprises a preservative effective amount of polyquaternium-1.

9. A method according to claim 8, wherein the composition contains polyquaternium-1 at a concentration of from 0.0001 to 0.001 w/v %.

10. A method according to claim 9, wherein the composition contains polyquaternium-1 at a concentration of 0.0005 w/v %.

11. A method according to claim 10, wherein the composition further comprises an antimicrobial enhancing amount of a buffer system having antimicrobial activity.

12. A method according to claim 11, wherein the buffer system comprises a borate/polyol complex.

13. A topical ophthalmic composition for treating dry eye, comprising 0.005 to 0.1 w/v % rimexolone and an ophthalmically acceptable vehicle therefor.

14. A topical ophthalmic composition according to claim 13, wherein the composition is a multi-dose suspension, and further comprises an effective amount of an antimicrobial preservative and an amount of polyvinyl pyrrolidone sufficient to suspend the rimexolone in the composition.

15. A topical ophthalmic composition according to claim 13, wherein the composition contains rimexolone at a concentration of 0.05 to 0.075 w/v %.

16. A topical ophthalmic composition according to claim 15, wherein the composition contains rimexolone at a concentration of 0.075 w/v %.

17. A topical ophthalmic composition according to claim 13, wherein the composition contains rimexolone at a concentration of 0.1 w/v %.

18. A topical ophthalmic composition according to claim 14, wherein the antimicrobial preservative comprises polyquaternium-1.

19. A topical ophthalmic composition according to claim 18, wherein the concentration of polyquaternium-1 in the composition is less than 0.001 w/v %.

20. A topical ophthalmic composition according to claim 19, wherein the concentration of polyquaternium-1 is 0.0005 w/v %.

21. A topical ophthalmic composition according to claim 20, wherein the composition further comprises an antimicrobial enhancing amount of a buffer system having antimicrobial activity.