Ophthalmic composition for the treatment of dry eye disease

Abstract

To provide compositions for treating patients meeting certain criteria for dry eye disease, as well as for treating patients for which certain symptoms of dry eye disease is particularly prevalent.SOLUTION: The invention provides ophthalmic compositions comprising 0.1% (w / v) cyclosporine dissolved in 1-(perfluorobutyl)pentane for use in the topical treatment of dry eye disease. The invention further provides kits comprising such compositions for the same use.SELECTED DRAWING: None

Claims

1. An ophthalmic composition for use in a method to increase tear production in a subject suffering from a dry eye disease (keratoconjunctivitis sicca), wherein the ophthalmic composition comprises 0.1% (w / v) cyclosporine and 1.0% (w / w) ethanol dissolved in 1-(perfluorobutyl)pentane, the suppression of tear production in the subject is caused by ocular inflammation associated with the dry eye disease (keratoconjunctivitis sicca), and the method comprises the step of topically administering the composition to the eye of a patient twice a day, per eye, as one drop having a volume of about 8 to 10 μl.

2. An ophthalmic composition for use in a method of treating ocular surface damage in a subject suffering from a dry eye disease (keratoconjunctivitis sicca), wherein the ophthalmic composition comprises 0.1% (w / v) cyclosporine and 1.0% (w / w) ethanol dissolved in 1-(perfluorobutyl)pentane, and the method comprises the step of topically administering the composition as one drop having a volume of about 8 to 10 μl to the eye of the subject twice a day, wherein the subject has a total ocular surface disease index (OSDI) score of 45 or higher.

3. The ophthalmic composition according to any one of claims 1 to 2, wherein the composition is administered topically to the surface of the eye.

4. The ophthalmic composition according to any one of claims 1 to 3, wherein the composition comprises 0.1% (w / v) cyclosporine, 1-(perfluorobutyl)pentane, and about 1.0% (w / w) ethanol.

5. The ophthalmic composition according to any one of claims 1 to 3, wherein the composition comprises 0.1% (w / v) cyclosporine dissolved in 1-(perfluorobutyl)pentane.

6. The ophthalmic composition according to any one of claims 1 to 5, wherein the subject is unresponsive or has an insufficient response to treatment with topical aqueous artificial tears.

7. The ophthalmic composition according to any one of claims 1 to 6, wherein the amount of cyclosporine administered as a single dose to each eye is approximately 8 to 10 μg.

8. The composition according to claim 2, wherein the treatment is for reducing damage to the ocular surface of the central corneal region and / or the lower corneal region.

9. The composition according to claim 2, wherein the composition is administered in one drop having a volume of 10 μl per dose and per eye.

10. The aforementioned subject is, i. Central corneal fluorescein staining (NEI scale) score of 2 or higher, ii. Lower corneal fluorescein staining (NEI scale) score of 2 or higher, iii. Total corneal fluorescein staining (NEI scale) score of 11 or higher The composition according to claim 2, having at least one or both eyes with any one or a combination of the following.

11. The aforementioned subject is, Total corneal fluorescein staining values ​​in the range of -10 to 15 (NEI scale), Central corneal fluorescein staining values ​​in the range of -2 to 3 (NEI scale), Total lysamine green conjunctival stain score in the range of -3 to 5. -Schirmer test score in the range of -2 to 8 mm without anesthesia, The composition according to claim 9, having at least one eye with any one or combination of criteria selected from the group consisting of the following.

12. The composition according to claim 2, wherein the subject has an unanesthetized Schirmer test score in the range of 3 to 7 mm in at least one eye.

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