Ophthalmic compositions

• US 5,951,971 A
• Filed: 12/17/1996
• Issued: 09/14/1999
• Est. Priority Date: 05/13/1992
• Status: Expired due to Term

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: Kuwano, Mitsuaki, Kawashima, Yoichi
• Primary Examiner(s): Kulkosky, Peter F.
• Application Number:
  US08/767,610
• Time in Patent Office: 1,001 Days
• Field of Search: 424/78.04, 514/885
• US Class Current: 424/78.04
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics
• 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 37/02 Immunomodulators
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

An ophthalmic composition particularly in the form of eye-drops suitable for the treatment of diseases of the eye and surrounding areas. The composition contains a cyclosporin and a surfactant selected from polyoxyethylene fatty acid esters, polyoxyethylene alkylphenyl ethers and polyoxyethylene alkyl ethers, or mixtures thereof.

Claims

1. An oil-free ophthalmic composition comprising:

(A) a cyclosporin,

(B) a surfactant selected from the group consisting of polyoxyethylene fatty acid esters, polyoxyethylene alkylphenyl ethers, and polyoxyethylene alkyl ethers, or mixtures thereof in an amount of from about 0.1% to about 3.0% (w/v); and

(C) purified water

the cyclosporin being in solution at a concentration of from about 0.01 to about 0.075% (w/v).

2. An ophthalmic composition of claim 1, further comprising a thickening agent.

3. An ophthalmic composition of claim 2 in which the thickening agent is selected from cellulose thickening agents, carboxyvinyl polymers, polyvinyl polymers, and polyvinylpyrrolidones.

4. An ophthalmic composition of claim 1 comprising:

1) from about 0.01 to about 0.075% (w/v) of cyclosporin A;

2) from about 0.15 to about 2.5% (w/v) of polyoxyl 40 stearate;

3) from about 0.1 to about 3.0% (w/v) of a cellulose thickening agent selected from hydroxypropyl methylcellulose and hydroxyethylcellulose; and

4) from about 0.0001 to about 0.01% (w/v) of an anti-oxidant selected from butylated hydroxytoluene and sodium thiosulfate.

5. An ophthalmic composition of claim 1 in which the cyclosporin is cyclosporin A.

6. An ophthalmic composition of claim 1 in a container appropriate for topical ophthalmic application of the composition.

7. A method of treating an autoimmune or inflammatory disease or condition of the eye or of the surrounding or associated organs or tissues in a subject in need thereof, which method comprises administering to said subject a composition of claim 1 topically to the eye.

8. An ophthalmic composition of claim 1 for use in a method of treating an autoimmune or inflammatory disease or condition of the eye or of the surrounding or associated organs or tissues in a subject in need thereof.

9. A method of claim 7 for treating an autoimmune disease or condition.

10. A method of claim 7, which comprises the suppression of organ transplant rejection.