Granted Patent B2

US 12,397,001 · App. 18/893,798 · Granted Aug 26, 2025

Inventors: Thorsteinn Loftsson (Reykjavik, IS); Zoltán Fülöp (Budapest, HU)

Assignee: Oculis Operations Sàrl

A61K31/573A61K9/0048A61K47/02A61K47/10A61K47/12A61K47/14A61K47/20A61K47/40A61P27/02A61P29/00

Abstract

Claims (37)

1. A method of treating ocular inflammation in a human subject in need thereof, the method comprising topically administering to an affected eye of the subject an effective amount of an aqueous ophthalmic composition comprising:

i) between 1% and 4% weight to volume (w/v) of dexamethasone;

ii) between 5% and 25% w/v of γ-cyclodextrin;

iii) between 0.1% and 0.5% w/v of sodium thiosulfate; and,

iv) water;

wherein the aqueous ophthalmic composition comprises a microsuspension comprising solid complexes of dexamethasone and γ-cyclodextrin;

wherein the aqueous ophthalmic composition is in a container made of plastic that allows oxidation of its contents; and,

wherein the aqueous ophthalmic composition has a pH of between 4.5 and 6.

2. The method of claim 1 , wherein the composition comprises 1.5% w/v of dexamethasone.

3. The method of claim 1 , wherein the composition comprises 14% w/v of γ-cyclodextrin.

4. The method of claim 1 , wherein the composition further comprises between 2.2% and 2.8% w/v of a poloxamer.

5. The method of claim 4 , wherein the composition comprises 2.5% w/v of the poloxamer.

6. The method of claim 4 , wherein the poloxamer is selected from the group consisting of poloxamer 101, poloxamer 105, poloxamer 108, poloxamer 122, poloxamer 123, poloxamer 124, poloxamer 181, poloxamer 182, poloxamer 183, poloxamer 184, poloxamer 185, poloxamer 188, poloxamer 212, poloxamer 215, poloxamer 217, poloxamer 231, poloxamer 234, poloxamer 235, poloxamer 237, poloxamer 238, poloxamer 282, poloxamer 284, poloxamer 288, poloxamer 331, poloxamer 333, poloxamer 334, poloxamer 335, poloxamer 338, poloxamer 401, poloxamer 402, poloxamer 403, poloxamer 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate.

7. The method of claim 6 , wherein the poloxamer is poloxamer 407.

8. The method of claim 1 , wherein the composition further comprises between 0% and 0.2% w/v of disodium edetate.

9. The method of claim 8 , wherein the composition comprises 0.1% w/v of disodium edetate.

10. The method of claim 1 , wherein the composition further comprises between 0% and 1% w/v of an electrolyte.

11. The method of claim 10 , wherein the electrolyte is selected from the group consisting of sodium chloride and potassium chloride.

12. The method of claim 10 , wherein the electrolyte is sodium chloride.

13. The method of claim 1 , wherein the composition comprises 0.3% w/v of sodium thiosulfate which corresponds to water-free sodium thiosulfate.

14. The method of claim 1 , wherein the sodium thiosulfate is sodium thiosulfate pentahydrate.

15. The method of claim 1 , wherein the solid complexes comprise microparticles with a diameter D 50 ranging from 1 μm to 10 μm.

16. The method of claim 1 , wherein the container is made of low-density polyethylene (LDPE).

17. A method of treating ocular inflammation in a human subject in need thereof, the method comprising topically administering to an affected eye of the subject an effective amount of an aqueous ophthalmic composition comprising:

i) between 1% and 4% weight to volume (w/v) of dexamethasone;

ii) between 5% and 25% w/v of γ-cyclodextrin;

iii) between 0.1% and 0.5% w/v of sodium thiosulfate; and,

iv) water;

wherein the aqueous ophthalmic composition comprises a microsuspension comprising solid complexes of dexamethasone and γ-cyclodextrin;

wherein the aqueous ophthalmic composition is in a container that allows oxidation of its contents and,

wherein the aqueous ophthalmic composition has a pH of between 4.5 and 6.

18. The method of claim 17 , wherein the composition further comprises between 0% and 0.2% w/v of disodium edetate.

19. The method of claim 18 , wherein the composition further comprises between 0% and 1% w/v of an electrolyte.

20. The method of claim 19 , wherein the composition further comprises between 2.2% and 2.8% w/v of a poloxamer.

21. The method of claim 20 , wherein the composition comprises 1.5% w/v of dexamethasone.

22. The method of claim 20 , wherein the composition comprises 14% w/v of γ-cyclodextrin.

23. The method of claim 17 , wherein the solid complexes comprise microparticles with a diameter D 50 ranging from 1 μm to 10 μm.

Assignments (3)

Priority Claims (2)

Continuity (2)

References Cited (188)