Claims for Patent: 10,751,325

Summary for Patent: 10,751,325

Title:	Stabilized oxymetazoline formulations and their uses
Abstract:	The present invention provides stabilized cream formulations of oxymetazoline and uses thereof. The present invention also provides a method of treating facial erythema associated with rosacea in a patient in need of such treatment, comprising topically administering once or twice daily to the site of erythema on the face of the patient a pharmaceutical composition comprising 0.5%, 1.0% or 1.5% oxymetazoline or a pharmaceutically acceptable salt thereof as the sole active ingredient.
Inventor(s):	Sarpotdar; Pramod (Rohnert Park, CA), Warner; Kevin (Anaheim, CA), Zhang; Steven (Newton, MA), Ahluwalia; Gurpreet (Tustin, CA), Kuang; Amy (Irvine, CA)
Assignee:	EPI HEALTH, LLC (Charleston, SC)
Application Number:	16/380,538
Patent Claims:	1. A method of treating persistent facial erythema associated with rosacea in an adult human patient in need of such treatment, said method comprising: administering topically, to one or more sites of erythema on the face of the adult human patient, a pharmaceutical composition comprising 1.0% w/w oxymetazoline hydrochloride as the sole active ingredient, wherein said pharmaceutical composition is a cream and said administering is carried out once daily. 2. The method of claim 1, wherein the pharmaceutical composition further comprises methylparaben, propylparaben, phenoxyethanol, sodium citrate, citric acid, disodium edetate, butylated hydroxytoluene, lanolin, medium chain triglycerides, diisopropyl adipate, oleyl alcohol, PEG-300, PEG-6 stearate, PEG-32 stearate, glycol stearate, cetostearyl alcohol, ceteareth-6, stearyl alcohol, ceteareth-25, and purified water. 3. The method of claim 2, wherein the pharmaceutical composition comprises about 1.0% w/w oxymetazoline HCl, about 0.2% w/w methylparaben, about 0.05% w/w propylparaben, about 0.8% w/w phenoxyethanol, about 0.3% w/w sodium citrate dihydrate, about 0.2% w/w anhydrous citric acid, about 0.01% w/w disodium edetate, about 0.05% w/w butylated hydroxytoluene, about 2% w/w anhydrous lanolin, about 7% w/w medium chain triglycerides, about 7% w/w diisopropyl adipate, about 7% w/w oleyl alcohol, about 4% w/w polyethylene glycol PEG-300, about 8% w/w polyethylene glycol PEG-6/polyethylene glycol PEG-32/glycol stearate, about 8% w/w cetostearyl alcohol, about 2% w/w ceteareth-6/stearyl alcohol, about 2% w/w ceteareth-25, and purified water. 4. The method of claim 1, wherein said administering results in an at least 2-grade improvement from baseline on Clinician's Erythema Assessment (CEA) scale, Subject Self-Assessment of Erythema (SSA), or both. 5. The method of claim 1, wherein said administering results in an at least 1-grade improvement from baseline on Clinician's Erythema Assessment (CEA) scale, Subject Self-Assessment of Erythema (SSA), or both. 6. The method of claim 1, wherein said administering once daily for 28 days results in a mean C.sub.max.+-.standard deviation (SD) of 66.4.+-.67.1 pg/mL in said adult human patient. 7. The method of claim 1, wherein said administering once daily for 28 days results in mean.+-.SD AUC.sub.0-24 of 1050.+-.992 pg-hr/mL in said adult human patient. 8. The method of claim 1, wherein said administering comprises topically applying a pea sized amount of the pharmaceutical composition to the one or more sites of erythema on the face of the adult human patient. 9. A method of treating persistent facial erythema associated with rosacea in an adult human patient in need of such treatment, said method comprising: administering topically, to the face of the adult human patient, a pharmaceutical composition comprising 1.0% w/w oxymetazoline hydrochloride as the sole active ingredient, wherein said pharmaceutical composition is a cream and wherein said administering is carried out once daily. 10. The method of claim 9, wherein said topically administering comprises applying a thin layer of said pharmaceutical composition over the entire face avoiding the eyes and lips. 11. The method of claim 9, wherein the pharmaceutical composition further comprises methylparaben, propylparaben, phenoxyethanol, sodium citrate, citric acid, disodium edetate, butylated hydroxytoluene, lanolin, medium chain triglycerides, diisopropyl adipate, oleyl alcohol, PEG-300, PEG-6 stearate, PEG-32 stearate, glycol stearate, cetostearyl alcohol, ceteareth-6, stearyl alcohol, ceteareth-25, and purified water. 12. The method of claim 9, wherein the pharmaceutical composition further comprises about 1.0% w/w oxymetazoline HCl, about 0.2% w/w methylparaben, about 0.05% w/w propylparaben, about 0 8% w/w phenoxyethanol, about 0.3% w/w sodium citrate dihydrate, about 0.2% w/w anhydrous citric acid, about 0.01% w/w disodium edetate, about 0.05% w/w butylated hydroxytoluene, about 2% w/w anhydrous lanolin, about 7% w/w medium chain triglycerides, about 7% w/w diisopropyl adipate, about 7% w/w oleyl alcohol, about 4% w/w polyethylene glycol PEG-300, about 8% w/w polyethylene glycol PEG-6/polyethylene glycol PEG-32/glycol stearate, about 8% w/w cetostearyl alcohol, about 2% w/w ceteareth-6/stearyl alcohol, about 2% w/w ceteareth-25, and purified water. 13. The method of claim 9, wherein said administering results in an at least 2-grade improvement from baseline on Clinician's Erythema Assessment (CEA) scale, Subject Self-Assessment of Erythema (SSA), or both. 14. The method of claim 9, wherein said administering once daily for 28 days results in a mean C.sub.max .+-.SD of 66.4.+-.67.1 pg/mL in said adult patient. 15. The method of claim 9, wherein said administering once daily for 28 days results in a mean AUC.sub.0-24 .+-.SD of 1050.+-.992 pg-hr/mL in said adult patient.