METHOD FOR REDUCING SIDE EFFECTS FROM ADMINISTRATION OF PHOSPHODIESTERASE-4 INHIBITORS
A method for altering the PK profile of a pharmaceutical formulation containing a PDE-4 inhibitor, such as roflumilast, to reduce the spike in Cmax. The spike in Cmax is reduced by topically administering the PDE-4 inhibitor in combination with one or more phosphate ester surfactants. Reducing the spike in Cmax will reduce gastrointestinal side effects and result in better patient compliance.
1 . A method for treating a patient suffering from vitiligo, comprising topically administering to said patient a composition comprising:
(i) roflumilast in an amount of 0.05%-1% w/w, and
(ii) a phosphate ester surfactant blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate in an amount of 1.0-25% w/w.
2 . The method of claim 1 , wherein said roflumilast is in an amount of 0.05% w/w.
3 . The method of claim 1 , wherein said roflumilast is in an amount of 0.15% w/w.
4 . The method of claim 1 , wherein said roflumilast is in an amount of 0.3% w/w.
5 . The method of claim 1 , wherein said composition is a cream, wherein said roflumilast is present in an amount 0.3% w/w, wherein said phosphate ester surfactant blend is present in an amount of 2.5%-20% w/w, and wherein said composition further comprises diethylene glycol monoethyl ether and water.
6 . The method of claim 5 , wherein said phosphate surfactant blend is present in an amount of 5%-15% w/w.
7 . The method of claim 6 , wherein said phosphate surfactant blend is present in an amount of 10% w/w.
8 . The method of claim 5 , wherein said composition further comprises hexylene glycol in an amount of 0.1-20% w/w.
9 . The method of claim 5 , wherein said composition further comprises at least one additional component selected from the group consisting of a solvent, moisturizer, preservative, pH adjusting solution, and skin penetration enhancer.
10 . The method of claim 1 , wherein said composition is a cream, wherein said phosphate surfactant blend is present in an amount of 2.5%-20% w/w, and wherein said composition further comprises diethylene glycol monoethyl ether and water.
11 . The method of claim 10 , wherein said phosphate surfactant blend is present in an amount of 5%-15% w/w.
12 . The method of claim 11 , wherein said phosphate surfactant blend is present in an amount of 10% w/w.
13 . The method of claim 10 , wherein said composition further comprises hexylene glycol in an amount of 0.1-20% w/w.
14 . The method of claim 10 , wherein said composition further comprises at least one additional component selected from the group consisting of a solvent, moisturizer, preservative, pH adjusting solution, and skin penetration enhancer.
15 . The method of claim 1 , wherein said composition is a cream, wherein said roflumilast is present in an amount 0.05% w/w, wherein said phosphate surfactant blend is present in an amount of 2.5%-20% w/w, and wherein said composition further comprises diethylene glycol monoethyl ether and water.
16 . The method of claim 15 , wherein said phosphate surfactant blend is present in an amount of 5%-15% w/w.
17 . The method of claim 16 , wherein said phosphate surfactant blend is present in an amount of 10% w/w.
18 . The method of claim 15 , wherein said composition further comprises hexylene glycol in an amount of 0.1-20% w/w.
19 . The method of claim 15 , wherein said composition further comprises at least one additional component selected from the group consisting of a solvent, moisturizer, preservative, pH adjusting solution, and skin penetration enhancer.
20 . A method for treating a patient suffering from vitiligo, comprising topically administering to said patient a composition comprising:
(i) roflumilast in an amount of 0.05%-1% w/w;
(ii) a surfactant;
(iii) a solvent; and
(iv) water.
21 . The method of claim 20 , wherein said roflumilast is in an amount of 0.3% w/w.
22 . The method of claim 20 , wherein said roflumilast is in an amount of 0.15% w/w.
23 . The method of claim 20 , wherein said roflumilast is in an amount of 0.05% w/w.
24 . The method of claim 20 , wherein the surfactant is a phosphate ester surfactant blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate in an amount of 1.0-25% w/w.
25 . The method of claim 20 , wherein the solvent is diethylene glycol monoethyl ether.
26 . The method of claim 20 , wherein said composition further comprises hexylene glycol in an amount of 0.1-20% w/w.
27 . The method of claim 20 , wherein said composition further comprises at least one additional component selected from the group consisting of a moisturizer, preservative, pH adjusting solution, and skin penetration enhancer.