Granted Patent B2

US 12,390,453 · App. 18/670,960 · Granted Aug 19, 2025

Inventor: David W. Osborne (Fort Collins, CO)

Assignee: ARCUTIS BIOTHERAPEUTICS, INC.

A61K31/44A61K9/0014A61K9/06A61K9/122A61K47/10A61K47/24A61P19/02A61K45/06

Abstract

Claims (32)

1. A pharmaceutical composition for topical administration comprising:

(i) roflumilast, wherein the roflumilast is in an amount of 0.05-1% w/w;

(ii) a phosphate ester surfactant blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate, wherein the phosphate ester surfactant blend is in an amount of 1.0-25% w/w; and

(iii) water;

wherein said pharmaceutical composition is in the form of a foam, and

wherein the C max of roflumilast from the topical composition is reduced relative to an oral roflumilast formulation marketed under the trademark DALIRESP®.

2. The composition of claim 1 , wherein said composition further comprises a propellant.

3. The composition of claim 2 , wherein said propellant is a blend of propane, isobutane, and n-butane.

4. The composition of claim 2 , wherein said phosphate ester surfactant blend is in an amount of 2% w/w.

5. The composition of claim 2 , wherein said composition further comprises diethylene glycol monoethyl ether.

6. The composition of claim 5 , wherein said diethylene glycol monoethyl ether is in an amount of 10-40% w/w.

7. The composition of claim 2 , wherein said roflumilast is in an amount of 0.3% w/w.

8. The composition of claim 2 , wherein said roflumilast is in an amount of 0.15% w/w.

9. The composition of claim 2 , wherein said roflumilast is in an amount of 0.05% w/w.

10. The composition of claim 2 , wherein said phosphate ester surfactant blend is in an amount sufficient to decrease a slope of the plasma concentration curve of the roflumilast between administration of said composition and Cmax.

11. The composition of claim 2 , wherein the plasma concentration curve of the roflumilast has no spike at C max .

12. A pharmaceutical composition for topical administration comprising:

(i) roflumilast, wherein the roflumilast is in an amount of 0.05-1% w/w;

(ii) a phosphate ester surfactant blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate, wherein the phosphate ester surfactant blend is in an amount of 1.0-25% w/w;

wherein said pharmaceutical composition is in the form of a foam, and

wherein the peak to trough ratio of roflumilast blood plasma concentration is less than 2 at steady state.

13. The composition of claim 12 , wherein said composition further comprises a propellant.

14. The composition of claim 13 , wherein said propellant is a blend of propane, isobutane, and n-butane.

15. The composition of claim 13 , wherein said phosphate ester surfactant blend is in an amount of 2% w/w.

16. The composition of claim 13 , wherein said composition further comprises diethylene glycol monoethyl ether.

17. The composition of claim 16 , wherein said diethylene glycol monoethyl ether is in an amount of 10-40% w/w.

18. The composition of claim 13 , wherein said roflumilast is in an amount of 0.3% w/w.

19. The composition of claim 13 , wherein said roflumilast is in an amount of 0.15% w/w.

20. The composition of claim 13 , wherein said roflumilast is in an amount of 0.05% w/w.

21. The composition of claim 13 , wherein the difference in a trough and an adjacent peak of the plasma concentration curve of the roflumilast at steady state is between about 4% and about 7%.

22. The composition of claim 13 , wherein the plasma concentration of the roflumilast plateaus after C max for 24 hours following administration.

23. The composition of claim 13 , wherein the peak to trough ratio is approximately 1 at steady state.

Assignments (2)

Continuity (5)

References Cited (190)