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 pharmaceutical composition for topical administration comprising:
(i) roflumilast, wherein the roflumilast is in an amount of 0.05-1.0% w/w;
(ii) water;
(iii) diethylene glycol monoethyl ether; and
(iv) an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate;
wherein the plasma half-life of the roflumilast is between 3 and 5 days after topical administration of the composition.
2. The composition according to claim 1 , wherein said composition comprises about 10% w/w of said emulsifier blend.
3. The composition according to claim 1 , wherein said composition comprises about 25% w/w diethylene glycol monoethyl ether.
4. The composition according to claim 1 , wherein said composition comprises w/w roflumilast.
5. The composition according to claim 4 , wherein said composition comprises about 10% w/w of said emulsifier blend.
6. The composition according to claim 4 , wherein said composition comprises about 25% diethylene glycol monoethyl ether.
7. A pharmaceutical composition for topical administration comprising:
(i) roflumilast in an amount of 0.05-1.0% w/w;
(ii) water qs ad 100% w/w;
(iii) diethylene glycol monoethyl ether in an amount of 10-30% w/w; and
(iv) an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate in an amount of 1.0-25% w/w;
wherein the composition is a foam or cream.
8. The composition according to claim 7 , wherein said composition is a foam, and wherein said composition comprises 25% w/w diethylene glycol monoethyl ether, 2% w/w emulsifier blend, white petrolatum, and isopropyl palmitate.
9. The composition according to claim 7 , wherein said composition is a cream, and wherein said composition comprises 25% w/w diethylene glycol monoethyl ether, 10% w/w emulsifier blend, 10.0% w/w white petrolatum, and 5.0% w/w isopropyl palmitate.