Topical roflumilast formulation having improved delivery and plasma half-life
The present invention is directed to methods for improving the therapeutic outcome of treatment with roflumilast. The therapeutic outcome is improved by consistent delivery and/or a longer plasma half-life of a topically administered roflumilast composition. The roflumilast composition preferably includes dicetyl phosphate, ceteth-10 phosphate, diethylene glycol I monoethyl ether, and/or hexylene glycol.
1. A method of treating a patient suffering from psoriasis comprising:
topically administering to said patient a pharmaceutical composition comprising a therapeutically effective amount of roflumilast, diethylene glycol monoethyl ether, and an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate,
wherein said composition comprises an amount of said emulsifier blend sufficient to increase the plasma half-life of roflumilast, and
wherein the plasma half-life of the roflumilast is between about 3 and about 5 days.
2. The method according to claim 1 , wherein said composition comprises 0.1% to 0.5% w/w roflumilast.
3. The method according to claim 2 , wherein said composition is a cream or foam.
4. The method according to claim 1 , wherein the plasma half-life of the roflumilast is between about 3 and about 4 days.
5. The method according to claim 1 , wherein said composition comprises about 10% w/w of said emulsifier blend.
6. The method according to claim 1 , wherein said composition comprises about 25% w/w diethylene glycol monoethyl ether.
7. The method according to claim 1 , wherein said roflumilast is in an amount of 0.1% to 0.5% w/w, said emulsifier blend is in an amount of 10% w/w and said diethylene glycol monoethyl ether is in an amount of 25% w/w, and wherein said composition is a cream.
8. The method according to claim 1 , wherein said roflumilast is in an amount of 0.1% to 0.5% w/w, said emulsifier blend is in an amount of 10% w/w and said diethylene glycol monoethyl ether is in an amount of 25% w/w, and wherein said composition is a foam.
9. A method of treating a patient suffering from inflammatory dermatoses comprising:
topically administering to said patient a pharmaceutical composition comprising a therapeutically effective amount of roflumilast, diethylene glycol monoethyl ether, and an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate,
wherein said composition comprises an amount of emulsifier blend sufficient to increase the plasma half-life of roflumilast, and
wherein the plasma half-life of the roflumilast is between about 3 and about 5 days.
10. The method according to claim 9 , wherein said composition comprises 0.05% to 1% w/w roflumilast.
11. The method according to claim 9 , wherein said composition is a cream or a foam.
12. The method according to claim 9 , wherein the plasma half-life of the roflumilast is between about 3 and about 4 days.
13. The method according to claim 9 , wherein said composition comprises about 10% w/w of said emulsifier blend.
14. The method according to claim 9 , wherein said composition comprises about 25% w/w diethylene glycol monoethyl ether.
15. The method according to claim 9 , wherein said patient is suffering from atopic dermatitis.
16. The method according to claim 15 , wherein said roflumilast is in an amount of 0.05% to 1% w/w, said emulsifier blend is in an amount of 10% w/w, said diethylene glycol monoethyl ether is in an amount of 25% w/w, and wherein said composition is a cream.
17. The method according to claim 9 , wherein said roflumilast is in an amount of 0.1% to 0.5% w/w, said emulsifier blend is in an amount of 10% w/w and said diethylene glycol monoethyl ether is in an amount of 25% w/w, and wherein said composition is a foam.
18. A method of treating a patient suffering from inflammatory dermatoses comprising:
topically administering to said patient once daily a composition comprising a therapeutically effective amount of roflumilast, diethylene glycol monoethyl ether, and an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate,
wherein said therapeutically effective amount of roflumilast is 0.05% to 1% w/w,
wherein said composition comprises an amount of said emulsifier blend sufficient to increase the plasma half-life of roflumilast,
wherein the plasma half-life of roflumilast is between about 3 and about 5 days, and
wherein the roflumilast remains at a therapeutically effective level after a patient misses one dose.
19. The method according to claim 18 , wherein said composition is a cream or foam.
20. The method according to claim 18 , wherein said emulsifier blend is in an amount of 10% w/w and said diethylene glycol monoethyl ether is in an amount of 25% w/w.