Granted Patent B2

US 12,589,069 · App. 18/086,286 · Granted Mar 31, 2026

Inventors: Mohannad Shawer (Lexington, MA); Eric Phillips (Ontario, NY); Martin J. Coffey (Buffalo Grove, IL)

Assignee: Bausch + Lomb Ireland Limited

A61K9/0048A61K9/14A61K9/146A61K31/56A61K31/573A61K47/02A61K47/06A61K47/10A61K47/32A61K47/38A61P27/02

Abstract

Claims (20)

1 . An ophthalmic suspension comprising an ophthalmic active ingredient suspended in a formulation vehicle, wherein the ophthalmic active ingredient is present as milled particles that have D v50 <1 μm, and the formulation vehicle comprises a suspending agent comprising a carboxyvinyl polymer and a particle size stabilizing agent comprising a non-ionic cellulose derivative, wherein the non-ionic cellulose derivative is hydroxypropylmethyl cellulose, the carboxyvinyl polymer is polycarbophil, the ophthalmic active ingredient is loteprednol etabonate, and the suspension comprises loteprednol etabonate at about 0.38 wt %, polycarbophil at 0.1-0.5 wt %, and hydroxypropylmethyl cellulose at 0.1-0.5 wt %.

2 . The suspension of claim 1 , which is storage stable for at least one year.

3 . The suspension of claim 1 , which is storage stable for at least two years.

4 . The suspension of claim 1 , wherein the loteprednol etabonate is present as particles that have D v90 <5 μm.

5 . The suspension of claim 1 , wherein the non-ionic cellulose derivative is hydroxypropylmethyl cellulose E3LV and is present at a concentration of at least 0.25%.

6 . The suspension of claim 1 , wherein the non-ionic cellulose derivative is hydroxypropylmethyl cellulose E4M.

7 . The suspension of claim 1 , wherein the poloxamer nonionic surfactant comprises poloxamer 407.

8 . The suspension of claim 1 , comprising hydroxypropylmethyl cellulose E3LV or hydroxypropylmethyl cellulose E4M, present at 0.15-0.25 wt %.

9 . The suspension of claim 1 , comprising hydroxypropylmethyl cellulose E4M at 0.15-0.25 wt %.

10 . The suspension of claim 1 , wherein the loteprednol etabonate is present as particles having D v90 <3 μm.

11 . The suspension of claim 1 , wherein the loteprednol etabonate is present as particles having D v90 <3 μm and D v50 <0.6 μm.

12 . The ophthalmic suspension of claim 1 , wherein upon storage of the suspension at 40° C. for 8.5 months, the particles will subsequently have a volume mean diameter of less than or equal to 1.23 micrometers measured using light diffraction.

13 . The ophthalmic suspension of claim 1 , wherein the suspension further comprises benzalkonium chloride at 0.001-0.01 wt %, edetate disodium dihydrate at 0.01-0.1 wt %, sodium chloride at 0.01-0.1 wt %, poloxamer nonionic surfactant at 0.1-1.0 wt %, and glycerin and propylene glycol at 0.1-2 wt %.

14 . The ophthalmic suspension of claim 13 , wherein the suspension further comprises a borate buffer at 0.01-1 wt %.

15 . A method of treating an ophthalmic inflammatory condition comprising administering to an eye of a patient in need of said treating a suspension comprising an ophthalmic anti-inflammatory active ingredient suspended in a formulation vehicle, wherein the ophthalmic anti-inflammatory active ingredient is present as milled particles that have D v50 <1 μm, and the formulation vehicle comprises a suspending agent comprising a carboxyvinyl polymer and a particle size stabilizing agent comprising a non-ionic cellulose derivative, wherein the non-ionic cellulose derivative is hydroxypropylmethyl cellulose, the carboxyvinyl polymer is polycarbophil, the ophthalmic active ingredient is loteprednol etabonate, and the suspension comprises loteprednol etabonate at about 0.38 wt %, polycarbophil at 0.1-0.5 wt %, and hydroxypropylmethyl cellulose at 0.1-0.5 wt %.

16 . The method of claim 15 , wherein the loteprednol etabonate is present as particles that have D v90 <5 μm and D v50 <1 μm.

17 . The method of claim 15 , wherein the suspension further comprises benzalkonium chloride at 0.001-0.01 wt %, edetate disodium dihydrate at 0.01-0.1 wt %, sodium chloride at 0.01-0.1 wt %, poloxamer nonionic surfactant at 0.1-1.0 wt %, and glycerin and propylene glycol at 0.1-2 wt %.

18 . The method of claim 17 , wherein the suspension further comprises a borate buffer at 0.01-1 wt %.

19 . The method of claim 15 , wherein the suspension comprises hydroxypropylmethyl cellulose E3LV or hydroxypropylmethyl cellulose E4M, present at 0.15-0.25 wt %.

20 . The method of claim 15 , wherein the suspension comprises hydroxypropylmethyl cellulose E4M at 0.15-0.25 wt %.

Assignments (8)

Continuity (4)

References Cited (98)