Claims for Patent: 12,589,069

Summary for Patent: 12,589,069

Title:	Ophthalmic suspension composition
Abstract:	A suspension includes an ophthalmic active ingredient suspended in a formulation vehicle including a suspending agent and a non-ionic cellulose derivative. The ophthalmic active agent is present as particles having Dv90<5 μm and Dv50<1 μm. The suspension may be administered to a patient for treating an ophthalmic inflammatory condition.
Inventor(s):	Mohannad Shawer, Eric Phillips, Martin J. Coffey
Assignee:	Bausch and Lomb Ireland Ltd
Application Number:	US18/086,286
Patent Claims:	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 Dv50<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 Dv90<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 Dv90<3 μm. 11. The suspension of claim 1, wherein the loteprednol etabonate is present as particles having Dv90<3 μm and Dv50<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 Dv50<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 Dv90<5 μm and Dv50<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 %.