IP Library › Granted Patent US 11,903,942
Granted Patent B2
US 11,903,942 · App. 18/125,517 · Granted Feb 20, 2024

Compositions and use of varenicline for treating dry eye

Inventors: Douglas Michael Ackermann, Jr. (Reno, NV); James Loudin (Houston, TX); Kenneth J. Mandell (Lexington, MA)
Assignee: Oyster Point Pharma, Inc.
A61K31/4995A61K9/007A61K9/0043A61K9/0048A61K9/08A61K31/439A61K31/4427A61K31/4439A61K31/4985A61K45/06
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Quick Facts
Patent No.
US 11,903,942
App. No.
18/125,517
Granted
Feb 20, 2024
Kind
B2
Abstract

Described herein are methods and pharmaceutical formulations for treating dry eye disease.

Claims (30)

1. A pharmaceutical formulation for local administration into a nasal cavity of an individual, the formulation comprising varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein varenicline in the formulation is in an amount of between 5 micrograms and 1000 micrograms, and the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL.

2. The pharmaceutical formulation of claim 1 , wherein the amount of varenicline in the formulation is between 5 micrograms and 100 micrograms.

3. The pharmaceutical formulation of claim 1 , wherein the amount of varenicline in the formulation is between 5 micrograms and 600 micrograms.

4. The pharmaceutical formulation of claim 1 , wherein the amount of varenicline in the formulation is between 5 micrograms and 500 micrograms per dose.

5. The pharmaceutical formulation of claim 1 , wherein the amount of varenicline in the formulation is between 5 micrograms and 75 micrograms per dose.

6. The pharmaceutical formulation of claim 1 , wherein the pharmaceutical formulation is a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm.

7. The pharmaceutical formulation of claim 1 , wherein the formulation comprises a solution of the varenicline or varenicline salt.

8. The pharmaceutical formulation of claim 7 , wherein the formulation is a liquid.

9. The pharmaceutical formulation of claim 8 , wherein the formulation is administered as a nasal spray.

10. The pharmaceutical formulation of according to claim 1 , wherein the formulation comprises a buffer.

11. The pharmaceutical formulation of claim 10 , wherein the buffer comprises a phosphate buffer or a phosphate-citrate buffer.

12. The pharmaceutical formulation of claim 11 , comprising a phosphate buffer with a pH of from around 5.0 to around 7.4.

13. The pharmaceutical formulation of claim 11 , comprising a phosphate buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.

14. The pharmaceutical formulation of to claim 1 , wherein the amount of varenicline in the formulation is about 0.5 mg per mL of the formulation.

15. The pharmaceutical formulation of claim 9 , wherein the amount of varenicline in the formulation is about 0.5 mg per mL of the formulation.

16. A nasal spray of a liquid pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, the varenicline in the formulation being in an amount of 5 micrograms to 1000 micrograms, and the concentration of varenicline in the formulation being between about 0.1 mg/mL and about 10 mg/mL.

17. The nasal spray of a liquid pharmaceutical formulation of claim 16 , wherein the amount of varenicline in the formulation is between 5 micrograms and 100 micrograms.

18. The nasal spray of a liquid pharmaceutical formulation of claim 16 , wherein the amount of varenicline in the formulation is between 5 micrograms and 600 micrograms.

19. The nasal spray of a liquid pharmaceutical formulation of according to claim 16 , wherein the amount of varenicline in the formulation is between 5 micrograms and 500 micrograms.

20. The nasal spray of a liquid pharmaceutical formulation of claim 16 , wherein the amount of varenicline in the formulation is between 5 micrograms and 75 micrograms.

21. The nasal spray of a liquid pharmaceutical formulation of claim 16 , the formulation comprising a phosphate buffer or a phosphate-citrate buffer.

22. The nasal spray of a liquid pharmaceutical formulation of claim 16 , the formulation comprising a phosphate buffer with a pH of from around 5.0 to around 7.4.

23. A nasal spray bottle containing a liquid pharmaceutical formulation for local administration into a nasal cavity of an individual, the formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, the varenicline in the formulation being in an amount of 5 micrograms to 1000 micrograms, and the concentration of varenicline in the formulation being between about 0.1 mg/mL and about 10 mg/mL.

24. The nasal spray bottle of claim 23 containing a liquid pharmaceutical formulation wherein the amount of varenicline in the formulation is 5 micrograms to 100 micrograms.

25. The nasal spray bottle of claim 23 , wherein each spray delivers about 50 microliters of the formulation.

26. The nasal spray bottle of claim 23 , wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate-citrate buffer.

27. The nasal spray bottle of claim 26 , wherein the pharmaceutical formulation comprises a phosphate buffer with a pH of from around 5.0 to around 7.4.

28. The nasal spray bottle of claim 26 , wherein the pharmaceutical formulation comprises a phosphate buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.

29. The nasal spray bottle of claim 25 , wherein each spray of about 50 microliters of the formulation contains from between 5 micrograms and 100 micrograms varenicline.

30. The nasal spray bottle of claim 25 , wherein each spray of about 50 microliters of the formulation contains from between 5 micrograms and 75 micrograms varenicline.

Continuity (7)
Continuation 17543505 · Dec 6, 2021
Continuation 16566237 · Sep 10, 2019
Continuation 15422382 · Feb 1, 2017
Continuation 14887248 · Oct 19, 2015
Provisional Application 62100844 · Jan 7, 2015
Provisional Application 62066280 · Oct 20, 2014
Related Publication 20230226052A1 · Jul 20, 2023
Cited By (2)
US 12,576,080 US 12,653,824