Topical roflumilast formulation having improved delivery and plasma half-life
Inventors
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12310956-B2
Publication Date
2025-05-27
Expiration Date
Abstract
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.
Core Innovation
The patent describes improved topical pharmaceutical compositions comprising roflumilast for treating inflammatory dermatoses. The compositions include roflumilast and diethylene glycol monoethyl ether together with an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate, and water. The compositions are administered once daily for the treatment.
A stated formulation problem addressed is inconsistent topical delivery associated with imperfect adherence, linked to systemic pharmacokinetic/pharmacodynamic considerations such as plasma half-life and forgiveness. The delivery objective is connected to achieving longer systemic exposure and terminal plasma half-life after topical dosing.
The patent further describes formulation improvements aimed at maintaining roflumilast physical and bioavailability characteristics by inhibiting crystal growth and precipitation/suspension changes. Reported comparative effects include reduced freeze-thaw precipitation with hexylene glycol and maintenance of particle size distribution, together with improved elimination kinetics and longer roflumilast plasma half-life from the combination of the phosphate ester self-emulsifying wax blend and hexylene glycol plus diethylene glycol monoethyl ether.
Claims Coverage
The partial content provides one independent claim. It covers a once-daily topical treatment of inflammatory dermatoses using a specific roflumilast-containing composition with defined components and amounts, and an emulsifier blend of specified constituents.
Once-daily topical inflammatory dermatoses treatment composition
A method of treating inflammatory dermatoses by topically administering a pharmaceutical composition comprising roflumilast (0.05–1.0% w/w), diethylene glycol monoethyl ether, an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate, and water, wherein the composition is administered once daily.
Defined roflumilast concentration range in the topical composition
The pharmaceutical composition includes roflumilast in an amount of 0.05–1.0% w/w.
Specific emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate
The pharmaceutical composition includes an emulsifier blend comprising cetostearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.
Diethylene glycol monoethyl ether inclusion in the topical composition
The pharmaceutical composition includes diethylene glycol monoethyl ether as a component of the once-daily topical formulation.
Across the independent claim, the main inventive concept is a once-daily topical composition for inflammatory dermatoses that combines roflumilast within a specified concentration range with diethylene glycol monoethyl ether and a specific emulsifier blend of cetostearyl alcohol, dicetyl phosphate, and ceteth-10 phosphate in water.
Stated Advantages
Improved roflumilast delivery and longer systemic exposure/terminal plasma half-life to increase forgiveness under imperfect adherence.
Reduced freeze-thaw precipitation effects and maintenance of particle size distribution for roflumilast.
Increased roflumilast plasma half-life and improved elimination kinetics with the described combination of components.
Documented Applications
Treatment of inflammatory dermatoses, including psoriasis.
Treatment of psoriasis lesions in intertriginous areas.
Interested in licensing this patent?