Inhibition of crystal growth of roflumilast
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Publication Number
US-12336983-B2
Publication Date
2025-06-24
Expiration Date
Abstract
Roflumilast crystals have been shown to increase in size during storage. The size of the roflumilast crystals can affect the bioavailability and efficacy of a pharmaceutical composition. The growth of roflumilast crystals can be inhibited during storage by including hexylene glycol in the composition. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in patient in need of such treatment.
Core Innovation
The problem addressed is that roflumilast crystals or particles can increase in size during storage, which can shift particle-size distribution and reduce topical bioavailability and/or efficacy. The description links this growth of suspended or precipitated roflumilast particles to diminished performance over shelf life.
The invention provides topical pharmaceutical compositions in which hexylene glycol is incorporated to inhibit roflumilast crystal growth in the composition during storage. By inhibiting crystal growth, the composition maintains roflumilast crystal habit/size and supports consistent topical delivery, thereby supporting improved bioavailability and efficacy.
The disclosure connects maintained crystal habit/size with improved bioavailability and efficacy under stability conditions, including freeze-thaw and temperature excursion conditions. The description also states that hexylene glycol is used in roflumilast pharmaceutical compositions, including topical formulations such as creams, foams, emulsions, gels, and suspensions.
Claims Coverage
The provided set includes one independent claim. It contains multiple inventive formulation elements directed to a topical pharmaceutical composition comprising roflumilast and hexylene glycol, with the specific functional effect of inhibiting roflumilast crystal growth over storage, in a cream or foam form.
Topical pharmaceutical composition with inhibited roflumilast crystal growth
A topical pharmaceutical composition comprising roflumilast in an amount of 0.005-2% (w/w) and hexylene glycol in an amount sufficient to inhibit roflumilast crystal growth in the composition, wherein the composition includes water, a surfactant, and a solvent and is in the form of a cream or foam.
Overall, the claim coverage centers on a topical cream or foam containing roflumilast (0.005-2% w/w) together with hexylene glycol present in an amount sufficient to inhibit roflumilast crystal growth, formulated with water, a surfactant, and a solvent.
Stated Advantages
Inhibits roflumilast crystal growth during storage.
Helps maintain consistent topical delivery by maintaining roflumilast crystal habit/size.
Improves topical bioavailability.
Improves topical efficacy.
Supports maintained bioavailability and efficacy under freeze-thaw and temperature excursion conditions.
Documented Applications
Topical pharmaceutical compositions, including creams, foams, emulsions, gels, and suspensions, for delivering roflumilast while inhibiting crystal growth during storage.
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