CYCLOSPORIN COMPOSITIONS FOR OCULAR ROSACEA TREATMENT
Disclosed herein are methods of treating ocular rosacea with cyclosporin A. Compositions and medicaments related thereto are also disclosed.
1 . A method of treating ocular rosacea comprising topically administering to a mammal in need thereof a composition comprising cyclosporin A at a concentration of from about 0.0001% (w/v) to less than about 0.05% (w/v).
2 . The method of claim 1 wherein the composition is an aqueous solution.
3 . The method of claim 1 wherein the concentration of cyclosporin A is from about 0.005% (w/v) to about 0.04% (w/v).
4 . The method of claim 2 wherein the concentration of cyclosporin A is from about 0.02% (w/v) to about 0.04% (w/v).
5 . The method of claim 2 wherein the composition contains no ethanol.
6 . The method of claim 2 wherein the composition contains no hyaluronic acid.
7 . The method of claim 2 wherein the composition contains no cyclodextrin A.
8 . The method of claim 6 wherein the composition contains no cyclodextrin.
9 . The method of claim 8 wherein the composition contains no ethanol.
10 . The method of claim 9 wherein the composition contains no hyaluronic acid.
11 . The method of claim 2 wherein the composition is administered only once a day.
12 . The method of claim 10 wherein the composition is administered only once a day.
13 . The method of claim 1 wherein topical administration of one 35 μL drop of said composition to each eye of a female New Zealand white rabbit provides to the corneas of said rabbit at least about 500 ng of cyclosporin A per gram of cornea of said rabbit at 30 minutes after said topical administration.
14 . The method of claim 12 , wherein the mammal is a human.
15 . The method of claim 1 wherein topical administration of one 35 μL drop of said composition to each eye of a female New Zealand white rabbit provides to the corneas of said rabbit at least about 1000 ng of cyclosporin A per gram of cornea of said rabbit at 30 minutes after said topical administration.
16 . The method of claim 1 wherein topical administration of one 35 μL drop of said composition to each eye of a female New Zealand white rabbit provides to the corneas of said rabbit at least about 1400 ng of cyclosporin A per gram of cornea of said rabbit at 30 minutes after said topical administration.
17 . The method of claim 1 wherein topical administration of one 35 μL drop of said composition to each eye of a female New Zealand white rabbit provides to the corneas of said rabbit at least about 17000 ng·hr of cyclosporin A per gram of cornea of said rabbit over a period of 24 hours after said topical administration.
18 . The method of claim 2 wherein topical administration of one 35 μL drop of said composition to each eye of a female New Zealand white rabbit provides to the conjunctivas of said rabbit at least about 3300 ng·hr of cyclosporin A per gram of conjunctiva of said rabbit over a period of 24 hours after said topical administration.
19 . The method of claim 2 wherein said composition is an aqueous solution containing from 0.005% (w/v) to about 0.04% (w/v) cyclosporin A, wherein topical administration of one 35 μL drop of said composition to each eye of a New Zealand rabbit provides at least about 17000 ng·hr of cyclosporin A per gram of cornea to the corneas of said rabbit as determined by:
topically administering said composition to each eye of each of 15 female New Zealand white rabbit test subjects; and
determining the amount of cyclosporin A in the corneas of three subjects at times of about 0.5 hours, about 2 hours, about 6 hours, about 12 hours, and about 24 after administration to said subject;
wherein the amount of cyclosporin A in the cornea is determined only once for each subject.
20 . The method of claim 2 wherein said composition is an aqueous solution containing from 0.005% (w/v) to about 0.04% (w/v) cyclosporin A, wherein topical administration of one 35 μL drop of said composition to each eye of a New Zealand rabbit provides at least about 6000 ng of cyclosporin A per gram of conjunctiva to the conjunctivas of said rabbit as determined by:
topically administering said composition to each eye of each of 15 female New Zealand white rabbit test subjects; and
determining the amount of cyclosporin A in the conjunctivas of three subjects at times of about 0.5 hours, about 2 hours, about 6 hours, about 12 hours, and about 24 after administration to said subject;
wherein the amount of cyclosporin A in the conjunctiva is determined only a single time for each subject.
21 . The method of claim 1 wherein the mammal is a human patient, and wherein less than 10% of human patients suffer burning or stinging when said composition is administered only once a day for a period of three months.
22 . The method of claim 1 wherein the composition contains a surfactant.
23 . A method of treating ocular rosacea comprising topically administering to a mammal a multi-use composition comprising cyclosporin A at a concentration of from about 0.0001% (w/v) to less than about 0.2% (w/v), and an effective amount of a preservative.
24 . The method of claim 61 wherein the preservative is an oxidizing preservative.
25 . The method of claim 61 wherein the preservative is a cationic preservative.