Claims for Patent: 11,058,677

Summary for Patent: 11,058,677

Title:	LFA-1 inhibitor formulations
Abstract:	The present invention provides formulations, methods and kits for the treatment of dry eye diseases. In particular, stabilized pharmaceutical compositions comprising the compound of Formula 1 are described herein for a variety of uses including the treatment of dry eye syndrome. In one aspect, methods and ingredients for improving the stability of compositions of the compound of Formula 1 are described.
Inventor(s):	Mary Newman, William HUNKE
Assignee:	Bausch and Lomb Ireland Ltd
Application Number:	US14/650,955
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,058,677
Patent Claims:	1. A composition comprising a compound of Formula 1: or a salt thereof, a pharmaceutically acceptable carrier, and a thiosulfate salt, wherein the composition has less than about 1% of total degradation products of the compound of Formula 1 when stored at a temperature of about 40° C. for a period of at least one month. 2. The composition of claim 1, wherein the pharmaceutically acceptable carrier is an aqueous carrier. 3. The composition of claim 2, wherein the thiosulfate salt is present in an amount of about 0.01% to about 0.5% w/v. 4. The composition of claim 2, wherein the thiosulfate salt is present in an amount of about 0.3% w/v. 5. The composition of claim 3, wherein the thiosulfate salt is sodium thiosulfate. 6. The composition of claim 5, wherein the composition is buffered to a pH of about 6.0 to about 8.5. 7. The composition of claim 6, wherein the compound of Formula 1 is present in an amount of about 1% to about 5% w/v. 8. The composition of claim 7, wherein the compound of Formula 1 is present in an amount of about 5% w/v. 9. The composition of claim 8, wherein the composition exhibits less than about 1% of total degradation products of the compound of Formula 1 upon storage at a temperature of about 40° C. for a time period selected from the group consisting of 2 months, 3 months, 4 months, 5 months, and 6 months. 10. The composition of claim 8, further comprising a sparged nitrogen gas. 11. The composition of claim 1, comprising: about 5% w/v of the compound of Formula 1; about 0.3% w/v thiosulfate salt; sodium chloride; and sodium phosphate, wherein the composition has a pH of about 7.0 to about 8.0. 12. The composition of claim 11, wherein the sodium phosphate is dibasic sodium phosphate. 13. A composition comprising: 4 to 10 w/v % compound of Formula 1: or a salt thereof; and 0.2 to 0.4% antioxidant, the antioxidant being sodium thiosulfate; wherein the composition is an aqueous solution with the compound of Formula 1 dissolved therein, and wherein the composition is suitable for topical administration to the eye. 14. A composition comprising: about 5 w/v % compound of Formula 1: or a salt thereof; about 0.3% w/v antioxidant, the antioxidant being sodium thiosulfate; sodium phosphate for buffering the compositions at a pH of 6.0 to 8.0; and sodium chloride for providing isotonicity to the composition; wherein the composition is an aqueous solution having the compound of Formula 1 dissolved therein, and wherein the composition is suitable for topical administration to the eye. 15. The composition of claim 13, wherein said thiosulfate salt is the primary antioxidant. 16. The composition of claim 13, further comprising a sparged inert gas. 17. The composition of claim 16, wherein the sparged inert gas is nitrogen. 18. The composition of claim 13, wherein the composition is buffered to a pH of about 7.5. 19. The composition of claim 1, wherein the composition comprises one or more antioxidants and a sparged inert gas. 20. The composition of claim 1, wherein the formulation expires in about 1-5 years when stored at or below ambient temperature. 21. The composition of claim 14, wherein the formulation expires in about 1-5 years when stored at or below ambient temperature.