Granted Patent
B2
US 12,576,080 · App. 19/169,843 · Granted Mar 17, 2026
Use of varenicline for treating ocular conditions
Inventors:
Douglas Michael Ackermann, Jr. (Reno, NV); James Loudin (Houston, TX); Kenneth J. Mandell (Lexington, MA)
A61K31/4995A61K9/0043A61K9/0048A61K9/007A61K9/08A61K31/439A61K31/4427A61K31/4439A61K31/4985A61K45/06
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Abstract
Described herein are methods and pharmaceutical formulations for treating dry eye disease.
Claims (29)
1 . A method of treating dry eye in a human comprising locally administering a spray of a liquid pharmaceutical formulation comprising between 25 micrograms and 50 micrograms of varenicline into a nostril twice daily, wherein the liquid pharmaceutical formulation comprises varenicline and the concentration of varenicline in the formulation is between about 0.5 mg/mL and about 1 mg/mL.
2 . The method of claim 1 , wherein the liquid pharmaceutical formulation does not include a preservative.
3 . The method of claim 1 , wherein the liquid pharmaceutical formulation comprises a phosphate buffer and the pH of the liquid pharmaceutical formulation is around 7.0.
4 . A method of treating dry eye in a human in need thereof comprising locally administering a spray of a liquid pharmaceutical formulation into a nostril, wherein the formulation comprises varenicline and one or more pharmaceutically acceptable inactive ingredients and the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, and wherein the amount of varenicline in the spray is between 5 micrograms and 100 micrograms.
5 . The method of claim 4 , wherein the concentration of varenicline in the formulation is between about 0.2 mg/mL and about 1 mg/mL.
6 . The method of claim 5 , wherein the concentration of varenicline in the formulation is between about 0.5 mg/mL and about 1 mg/mL.
7 . The method of claim 4 , wherein the amount of varenicline in the spray is between 5 micrograms and 50 micrograms.
8 . The method of claim 7 , wherein the concentration of varenicline in the formulation is between about 0.2 mg/mL and about 1 mg/mL.
9 . The method of claim 8 , wherein the concentration of varenicline in the formulation is between about 0.5 mg/mL and about 1 mg/mL.
10 . The method of claim 9 , wherein the formulation does not include a preservative.
11 . The method of claim 4 , wherein the amount of varenicline in the spray is between 25 micrograms and 50 micrograms.
12 . The method of claim 11 , wherein the concentration of varenicline in the formulation is between about 0.2 mg/mL and about 1 mg/mL.
13 . The method of claim 12 , wherein the concentration of varenicline in the formulation is between about 0.5 mg/mL and about 1 mg/mL.
14 . The method of claim 13 , wherein the formulation does not include a preservative.
15 . The method of claim 4 , wherein the local administration is repeated in a second nostril.
16 . The method of claim 8 , wherein the local administration is repeated in a second nostril.
17 . The method of claim 10 , wherein the local administration is repeated in a second nostril.
18 . The method of claim 12 , wherein the local administration is repeated in a second nostril.
19 . The method of claim 4 , wherein the liquid pharmaceutical formulation comprises a phosphate buffer.
20 . The method of claim 19 , wherein the liquid pharmaceutical formulation has a pH around 7.0.
21 . The method of claim 10 , wherein the liquid pharmaceutical formulation comprises a phosphate buffer.
22 . The method of claim 21 , wherein the liquid pharmaceutical formulation has a pH around 7.0.
23 . The method of claim 13 , wherein the liquid pharmaceutical formulation comprises a phosphate buffer.
24 . The method of claim 23 , wherein the liquid pharmaceutical formulation has a pH around 7.0.
25 . The method of claim 24 , wherein the liquid pharmaceutical formulation does not include a preservative.
26 . The method of claim 4 , wherein the formulation comprises a phosphate-citrate buffer, and wherein the formulation has a pH from around 5.0 to around 6.0.
27 . The method of claim 10 , wherein the formulation comprises a phosphate-citrate buffer, and wherein the formulation has a pH from around 5.0 to around 6.0.
28 . The method of claim 14 , wherein the formulation comprises a phosphate-citrate buffer, and wherein the formulation has a pH from around 5.0 to around 6.0.
29 . The method of claim 14 , wherein the local administration is repeated in a second nostril.
Continuity (8)
Provisional Application
62100844
· Jan 7, 2015
Provisional Application
62066280
· Oct 20, 2014
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