Ophthalmic formulations

• US 6,953,776 B2
• Filed: 11/21/2003
• Issued: 10/11/2005
• Est. Priority Date: 04/07/2000
• Status: Expired due to Term

• Current Assignee: Laboratoire Medidom Sa
• Original Assignee: Laboratoire Medidom Sa
• Inventors: Di Napoli, Guido
• Primary Examiner(s): Weber, Jon
• Assistant Examiner(s): Snedden, Sheridan
• Application Number:
  US10/721,007
• Publication Number:
  US 20040106546A1
• Time in Patent Office: 690 Days
• Field of Search: 514 9- 11, 514/54, 514/2, 435/6, 435/7.1, 435/69, 530/317, 530/321
• US Class Current: 514/20.5
• CPC Class Codes: A61K 38/13 Cyclosporins
• 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 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• 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
• 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 37/06 Immunosuppressants, e.g. drugs for graft rejection

Abstract

A topical ophthalmic formulation in the form of an aqueous solution comprising a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80 is described.

Claims

1. A method for preparing an aqueous formulation for topical ophthalmic use comprising the step of associating a cyclosporin with hyaluronic acid or one of its salts and polysorbate 80.

2. The method for preparing an aqueous formulation according to claim 1, wherein the formulation comprises 0.02 to 2% by weight of cyclosporin, 0.01 to 2% by weight of hyaluronic acid or one of its salts, and 0.5 to 40% by weight of polysorbate 80, based on the formulation'"'"'s total weight.

3. The method for preparing an aqueous formulation according to claim 1, wherein the cyclosporin is a cyclosporin A.

4. The method for preparing an aqueous formulation according to claim 1, wherein the hyaluronic acid or its salt has a weight-average molecular weight not inferior to 1,300,000 daltons.

5. The method for preparing an aqueous formulation according to claim 4, wherein the hyaluronic acid or its salt has a weight-average molecular weight situated in the region from 1,300,000 to 3,000,000 daltons.

6. The method for preparing an aqueous formulation according to claim 1, wherein the hyaluronic acid is present as alkali metal or alkaline-earth metal hyaluronate.

7. The method for preparing an aqueous formulation according to claim 6, wherein the hyaluronic acid is present as sodium hyaluronate.

8. A method for treating conditions selected from the group consisting of keratoconjunctivitis sicca (KCS), Sjö

gren'"'"'s syndrome, dry-eye syndrome and chronic vernal keratoconjunctivitis comprising the step of administering a formulation of a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80.

9. A method for post-operative prophylactic treatment in keratoplasty comprising the step of using a formulation comprising a cyclosporin, hyaluronic acid or one of its salts, and polysorbate 80.