Claims for Patent: 8,513,249

Summary for Patent: 8,513,249

Title:	Methods and compositions for safe and effective treatment of erythema
Abstract:	Improved methods and compositions for safe and effective treatment of erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.4% to about 0.6% by weight of brimonidine and a pharmaceutically acceptable carrier.
Inventor(s):	Graeber; Michael (Lawrenceville, NJ), Loesche; Christian (Valbonne, FR), Freidenreich; Philip (Yardley, PA), Liu; Yin-Sang (Princeton, NJ), Leoni; Matthew J. (Hampton, NJ)
Assignee:	Galderma Laboratories, L.P. (Fort Worth, TX)
Application Number:	13/456,976
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,513,249
Patent Claims:	1. A method of treating erythema or a symptom associated therewith in a subject, comprising topically administering to a skin area affected by the erythema or the symptom a topical composition comprising, relative to the total weight of the composition, 0.4% to 0.6% by weight of brimonidine, and a pharmaceutically acceptable carrier, wherein the topical administration effects a serum or plasma profile of brimonidine having a mean C.sub.max of about 54.+-.28 pg/mL or less and a mean AUC.sub.0-24 hr hr of about 568.+-.277 pg.hr/mL or less. 2. The method of claim 1, wherein the erythema is erythema of rosacea. 3. The method of claim 1, further comprising providing to the subject at least one additional treatment and medication for erythema or the symptom associated therewith. 4. The method of claim 1, wherein the topical composition is administered to the skin area once daily. 5. The method of claim 1, wherein the topical administration of the topical composition to the skin area results in more reduction of the erythema or the symptom compared to a vehicle control as measured by a 12 hour success profile evaluated on both Clinician's Erythema Assessment scores and Patient's Self Assessment scales, wherein the 12 hour success profile comprises an effect of 1-grade improvement of the erythema or the symptom and about 1 hour to about 8 hours of 2-grade improvement of the erythema or the symptom. 6. The method of claim 5, wherein the erythema or the symptom is facial erythema associated with rosacea, and the 12 hour success profile comprises an effect of 1-grade improvement of the facial erythema and about 3 hours to about 6 hours of 2-grade improvement of the facial erythema. 7. The method of claim 1, wherein the brimonidine is brimonidine tartrate. 8. The method of claim 7, wherein the topical composition comprises about 0.5% by weight of brimonidine tartrate relative to the total weight of the composition. 9. The method of claim 1, wherein the topical composition further comprises about 0.50% to about 2.0% by weight of a gelling agent relative to the total weight of the composition, and the gelling agent comprises a carbomer. 10. The method of claim 9, wherein the carbomer is selected from the group consisting of carbomer 934P, carbomer 974P, and carbomer 980. 11. The method of claim 1, wherein the topical composition further comprises about 0.04% to about 0.08% by weight of water dispersible form of titanium dioxide relative to the total weight of the composition. 12. The method of claim 1, wherein the topical composition further comprises a preservative selected from the group consisting of sodium benzoate, phenoxyethanol, benzyl alcohol, methylparaben, imidazolidinyl urea and diazolidinyl urea. 13. The method of claim 1, wherein the topical composition further comprises about 5.0% to about 15.0% by weight of at least one polyol relative to the total weight of the composition. 14. A method of producing a packaged product for treating erythema or a symptom associated therewith in a subject, comprising: (1) obtaining a topical composition comprising, relative to the total weight of the composition, 0.4% to 0.6% by weight of brimonidine, and a pharmaceutically acceptable carrier; (2) devising instructions for topically administering the topical composition to a skin area affected by the erythema or the symptom to obtain the treatment, and (3) providing the topical composition and the instructions in a unified package for the subject, wherein the topical administration effects a serum or plasma profile of brimonidine having a mean C.sub.max of about 54.+-.28 pg/mL or less and a mean AUC.sub.0-24 hr of about 568.+-.277 pg.hr/mL or less. 15. A topical composition for treating erythema or a symptom associated therewith in a subject, the composition comprising, relative to the total weight of the composition: 0.4% to 0.6% by weight of brimonidine; and a pharmaceutically acceptable carrier, wherein the topical administration of the topical gel composition to a skin area affected by the erythema or the symptom effects a serum or plasma profile of brimonidine having a mean C.sub.max of about 54.+-.28 pg/mL or less and a mean AUC.sub.0-24 hr of about 568.+-.277 pg.hr/mL or less. 16. The topical gel composition of claim 15, wherein the brimonidine is brimonidine tartrate. 17. The topical gel composition of claim 16, comprising about 0.5% by weight of brimonidine tartrate relative to the total weight of the composition. 18. The topical gel composition of claim 15, further comprising about 0.50% to about 2.0% by weight of a gelling agent relative to the total weight of the composition, and the gelling agent comprises a carbomer. 19. The topical gel composition of claim 15, wherein the topical composition further comprises about 5.0% to about 15.0% by weight of one polyol relative to the total weight of the composition. 20. The method of claim 1, wherein the erythema or the symptom associated therewith is facial erythema associated with rosacea, and the topical composition comprises about 0.5% by weight of brimonidine tartrate relative to the total weight of the composition. 21. The topical composition of claim 15, wherein the topical administration of the topical composition to the skin area results in more reduction of the erythema or the symptom compared to a vehicle control as measured by a 12 hour success profile evaluated on both Clinician's Erythema Assessment scores and Patient's Self Assessment scales, wherein the 12 hour success profile comprises an effect of 1-grade improvement of the erythema or the symptom and about 1 hour to about 8 hours of 2-grade improvement of the erythema or the symptom. 22. The topical composition of claim 21, wherein the erythema or the symptom is facial erythema associated with rosacea, and the 12 hour success profile comprises an effect of 1-grade improvement of the facial erythema and about 3 hours to about 6 hours of 2-grade improvement of the facial erythema.