Stable Aqueous Cyclosporin Compositions

• US 20090286718A1
• Filed: 11/17/2008
• Published: 11/19/2009
• Est. Priority Date: 01/04/2008
• Status: Abandoned Application

• Current Assignee: Alcon Pharmaceuticals Limited (Alcon Incorporated)
• Original Assignee: Sirion Therapeutics, Inc. (Bausch Health Cos., Inc.)
• Inventors: STRINGER, William Francis
• Application Number:
  US12/272,445
• Publication Number:
  US 20090286718A1
• Time in Patent Office: Days
• US Class Current: 514/1.100
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• 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 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

An aqueous ophthalmic composition is disclosed. The composition may comprise a cyclosporin in an amount from about 0.001 to about 1%, glycerin, and purified water, wherein the composition is substantially free of NaCl and sodium bisulfite or sodium metabisulfite. The composition is useful for the treatment of ocular conditions.

Claims

1. An aqueous ophthalmic composition comprising:

(a) a cyclosporin in an amount of from about 0.001% to about 1%;

(b) glycerin in an amount between about 0.1% and about 5%; and

(c) purified water;

(d) wherein the composition contains less than about 0.3% sodium chloride and less than about 0.04% sodium metabisulfite.

2. The aqueous ophthalmic composition of claim 1, wherein the pH of the aqueous ophthalmic composition is between about 6.0 and about 7.5.

3. The aqueous ophthalmic composition of claim 1, wherein the pH of the aqueous ophthalmic composition is about 6.5.

4. The aqueous ophthalmic composition of claim 1, wherein the composition is substantially free of sodium chloride.

5. The aqueous ophthalmic composition of claim 1, wherein the composition is substantially free of sodium metabisulfite.

6. The aqueous ophthalmic composition of claim 1, wherein the composition is substantially free of sodium chloride and sodium metabisulfite and is stable.

7. The aqueous ophthalmic composition of claim 1, further comprising a polyoxyethylene sorbitan fatty acid ester and a polyoxyethylene fatty acid ester in a total amount between about 7% and about 8%.

8. The aqueous ophthalmic composition of claim 7, wherein the polyoxyethylene sorbitan fatty acid ester and the polyoxyethylene fatty acid ester each have a HLB number between about 15 to about 17.

9. The aqueous ophthalmic composition of claim 7, wherein the polyoxyethylene sorbitan fatty acid ester is present in an amount between about 0.50% and about 0.55% and the polyoxyethylene fatty acid ester is present in an amount of about 7%.

10. The aqueous ophthalmic composition of claim 7, wherein the polyoxyethylene sorbitan fatty acid ester is polyoxyethylene 20 sorbitan monooleate.

11. The aqueous ophthalmic composition of claim 7, wherein the polyoxyethylene fatty acid ester is polyoxyethylene 40 monostearate.

12. The aqueous ophthalmic composition of claim 1, further comprising ethanol in an amount from about 0.2% to about 0.5%.

13. The aqueous ophthalmic composition of claim 1, further comprising boric acid in an amount from about 0.01% to about 0.2%.

14. The aqueous ophthalmic composition of claim 1, further comprising sorbic acid in an amount from about 0.01 to about 0.5%.

15. The aqueous ophthalmic composition of claim 14, wherein the sorbic acid is in an amount from about 0.2 to about 0.3% and the composition is stable.

16. The aqueous ophthalmic composition of claim 1, further comprising ethylene diamine tetraacetic acid in an amount from about 0.01% to about 1%.

17. The aqueous ophthalmic composition of claim 1, further comprising a therapeutically effective amount of a member selected from the group consisting of an antihistamine, a mast cell stabilizer, a steroidal anti-inflammatory agent, a non-steroidal anti-inflammatory agent, and mixtures thereof.

18. A method of treating an ocular condition comprising contacting ocular tissue with an aqueous composition comprising:

(a) a cyclosporin in an amount of from about 0.001% to about 1%;

(b) glycerin in an amount between about 0.1% to about 5%; and

(c) purified water;

(d) wherein the composition contains less than about 0.3% sodium chloride and less than about 0.04% sodium metabisulfite.

19. The method of claim 18, wherein the composition further comprises sorbic acid in an amount from about 0.01 to about 0.5% and the composition is stable.

20. An aqueous ophthalmic composition comprising:

(a) a cyclosporin in an amount of 0.1%;

(b) glycerin in an amount of 1.15%;

(c) polyoxy 40 stearate in an amount of 7%;

(d) EDTA in an amount of 0.1%;

(e) boric acid in an amount of 0.095%;

(f) sorbic acid in an amount of 0.22%;

(g) polysorbate 80 in an amount of 0.537%; and

(h) ethyl alcohol in an amount of 0.395%.

(i) wherein the composition contains less than about 0.3% sodium chloride and less than about 0.04% sodium metabisulfite.