Method for reducing side effects from administration of phosphodiesterase-4 inhibitors
AssigneeArcutis Biotherapeutics, Inc.
InventorsDavid W. Osborne, Howard Welgus
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Abstract
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.
Claims43
A method for reducing gastrointestinal side effects of roflumilast relative to an oral roflumilast formulation marketed under the trademark DALIRESP®, 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.
A method for reducing gastrointestinal side effects of roflumilast relative to an oral roflumilast formulation marketed under the trademark DALIRESP®, 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, wherein the peak to trough ratio of roflumilast blood plasma concentration is less than 2 after multiple daily administrations, and wherein the patient is suffering from an inflammatory dermatoses.
A method for reducing gastrointestinal side effects of a topical roflumilast composition, comprising adding a phosphate ester surfactant blend in an amount of 1.0-25% w/w to a composition comprising roflumilast in an amount of 0.05%-1% w/w and a pharmaceutically acceptable solvent, wherein the phosphate ester surfactant blend comprises cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.
Dependencies are inferred from the claim text.