38 results about "Roflumilast" patented technology

This invention relates to the treatment of a neuropsychiatric disorder, such as schizophrenia or Parkinson's disease, by administration (for example, transdermally) of tilivapram, zatolmilast, roflumilast, or a pharmaceutically acceptable salt thereof.

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.

This invention relates to the treatment of a neuropsychiatric disorder, such as schizophrenia or Parkinson's disease, by administration (for example, transdermally) of tilivapram, zatolmilast, roflumilast, or a pharmaceutically acceptable salt thereof.

This method involves treating a patient's skin condition or disease by topically applying a pharmaceutical composition containing roflumilast. Treatment methods include once-daily application of the roflumilast composition for a period of time, followed by twice-weekly application of the roflumilast composition as a maintenance dosing regimen.

Ophthalmic pharmaceutical formulations of the phosphodiesterase-4 inhibitor, roflumilast formulated with optimized viscosity and are suitable for intravitreal or other forms of ocular administration. The compositions can improve drug administration and absorption, distribution, metabolism, and excretion (ADME) properties. The ophthalmic pharmaceutical formulations can be administered via intravitreal injection resulting in the formation of a depot in the vitreous. The depot can remain in the vitreous for a prolonged period of time resulting in therapeutic drug levels over this period of time and improved durability.

The present invention is directed to a method 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 comprises dicetyl phosphate, ceteth-10 phosphate, diethylene glycol monoethyl ether, and / or hexylene glycol.

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.

The present invention is directed to an aerosol foam composition comprising roflumilast, an emulsifier blend containing cetearyl alcohol, dicetyl phosphate, and ceteareth-10 phosphate and a hydrocarbon propellant. The aerosol foam composition is preferably an oil in water emulsion. The propellant is a mixture of liquefied hydrocarbon gases preferably a propane / isobutane / butane blend. The hydrocarbon propellant results in an aerosol foam which is stable, has consistent physical properties, excellent aesthetics, and no discernable degradation after long term or accelerated storage conditions.

The present invention is directed to a method of treating a fungal infection comprising administering topically, to a subject in need thereof, an anti-fungal effective amount of roflumilast. Preferably, topically administered roflumilast is used to treat fungal infections, fungal growth of and / or hypersensitivity to the fungi Malassezia spp. Patients may also be suffering from seborrheic dermatitis, dandruff, dupilumab facial redness, Tinea versicolor, Pityriasis versicolor, Tinea circinata, Tinea pedis, Tinea unguium, Tinea manus, Tinea cruris, Tinea corporis, Tinea faciei, Tinea capitis, and / or Tinea incognito. Topically administered roflumilast is a quick and effective antifungal agent and presents a viable alternative to current antifungal treatments.

Methods of treating a patient suffering from one or more of epidermal disorders of persistent inflammation—cell kinetics and differentiation disorders, epidermal disorders of persistent inflammation—altered reactivity disorders, disorders of the lips, oral, or vaginal mucosa, epidermal disorders of cohesion—vesicular and bullous disorders, cutaneous lymphomas, skin manifestations of rheumatologic diseases, hypomelanoses and hypermelanoses, or skin manifestations related to oncology treatments. The methods include topical administration of a pharmaceutical composition comprising a therapeutically effective amount of roflumilast.

The present invention is directed to an aerosol foam composition comprising roflumilast, an emulsifier blend containing cetearyl alcohol, dicetyl phosphate, and ceteareth-10 phosphate and a hydrocarbon propellant. The aerosol foam composition is preferably an oil in water emulsion. The propellant is a mixture of liquefied hydrocarbon gases preferably a propane / isobutane / butane blend. The hydrocarbon propellant results in an aerosol foam which is stable, has consistent physical properties, excellent aesthetics, and no discernable degradation after long term or accelerated storage conditions.

Topical pharmaceutical compositions comprising roflumilast and solvents that are capable of dissolving high amounts of roflumilast. The pharmaceutical compositions are capable of dissolving high amounts of roflumilast relative to other commonly used solvents in approved topical pharmaceutical compositions. The solvents are particularly useful when combined with water to maintain high levels of dissolved roflumilast, which is highly insoluble in water.

Disclosed is a pharmaceutical composition for preventing or treating psoriasis and atopic dermatitis. The pharmaceutical composition for preventing or treating psoriasis and atopic dermatitis according to one embodiment comprises: a phosphodiesterase-4 inhibitor including at least one of a phosphodiesterase-4 inhibitory component or a pharmaceutically acceptable salt thereof; and an active ingredient including at least one of octenidine or an octenidine salt, wherein the phosphodiesterase-4 inhibitory component may include at least one among roflumilast, dipamilast, and tanimilast.

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 monoethyl ether, and / or hexylene glycol.

The present invention relates to methods of treating ocular inflammatory diseases by administering ophthalmic pharmaceutical compositions of roflumilast. Administration of ophthalmic pharmaceutical compositions of roflumilast can provide significant immunomodulatory and anti-inflammatory activity relative to existing immunomodulatory, immunosuppressant, or non-steroidal anti-inflammatory therapies, including corticosteroids and antihistamines, while also providing an improved safety and convenience profile relative to one or both agents.

A method of treating an anterior or vitreous atrial ocular disease by topically administering an ophthalmic pharmaceutical composition of roflumilast to the ocular surface of the eye of a patient. The methods involve topically administering an ophthalmic pharmaceutical composition of roflumilast to the ocular surface of a patient three or four times per day at a higher frequency and higher concentration, the use of which involves a higher concentration and lower frequency dosing regimen compared to other therapeutic regimens, which can provide significant therapeutic activity to the anterior and vitreous atrial chambers of the eye.

The present invention relates to a topical composition comprising roflumilast or a pharmaceutically acceptable salts thereof. Further the invention relates to a process of preparing the composition and its method of use for treating skin disorder. The present invention particularly relates to a topical foam composition comprising roflumilast or a pharmaceutically acceptable salts thereof.

The low aqueous solubility of roflumilast in parenteral preparations and topical emulsions, suspensions, gels or solutions can be improved by including a blend of water-miscible solvents in the pharmaceutical composition. The blend of water-miscible solvents can include diethylene glycol monoethyl ether (Tradename Transcutol®); abbreviated DEGEE) and water. The ratio of diethylene glycol monoethyl ether to water is from 1:10 to 20:1. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in a patient in need of such treatment.

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.

Methods of administering ophthalmic pharmaceutical formulations of the phosphodiesterase-4 inhibitor, roflumilast, for treating patients with ocular comorbidities of autoimmune disorder, including dry eye disease. The methods include selecting a patient previously diagnosed with an autoimmune disorder and administering an ophthalmic pharmaceutical composition comprising roflumilast to the patient to treat the ocular comorbidity of the autoimmune disorder. The method can result in a reduction of a total lissamine green conjunctival staining score or a reduction in total corneal fluorescein staining score relative to baseline.

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.

The present invention is directed to a method of treating a fungal infection comprising administering topically, to a subject in need thereof, an anti-fungal effective amount of roflumilast. Preferably, topically administered roflumilast is used to treat fungal infections, fungal growth of and / or hypersensitivity to the fungi Malassezia spp. Patients may also be suffering from seborrheic dermatitis, dandruff, dupilumab facial redness, tinea versicolor, pityriasis versicolor, tinea circinata, tinea pedis, tinea unguium, tinea manus, tinea cruris, tinea corporis, tinea faciei, tinea capitis, and / or tinea incognito. Topically administered roflumilast is a quick and effective antifungal agent and presents a viable alternative to current antifungal treatments.

Methods of treating anterior or vitreous chamber ocular diseases by administering ophthalmic pharmaceutical compositions of roflumilast topically to the ocular surface of the eye of a patient. The met

An improved method is provided for treating a patient having a disorder responsive to PDE-4 inhibition by administering roflumilast. The improvement involves administering the roflumilast topically in a composition having a roflumilast release profile that produces in the patient a flattened plasma concentration time curve and a reduced Cmax relative to oral administration of a PDE4-inhibiting amount of roflumilast. Such disorders include inflammatory disorders such as inflammatory dermatoses, including psoriasis, atopic dermatitis and seborrheic dermatitis. Such disorders also include inflammatory diseases in a variety of organs, especially the lungs (asthma, COPD). Because of reduced side effects with topical administration due to the improved pharmacokinetics (PK) characteristics, it may be possible to provide higher systemic exposures (AUCs) with topical administration, resulting in greater therapeutic efficacy than with the oral route of administration.

Methods of treating a patient suffering from one or more of epidermal disorders of persistent inflammation—cell kinetics and differentiation disorders, epidermal disorders of persistent inflammation—altered reactivity disorders, disorders of the lips, oral, or vaginal mucosa, epidermal disorders of cohesion—vesicular and bullous disorders, cutaneous lymphomas, skin manifestations of rheumatologic diseases, hypomelanoses and hypermelanoses, or skin manifestations related to oncology treatments. The methods include topical administration of a pharmaceutical composition comprising a therapeutically effective amount of roflumilast.

An inhalation formulation for treating an IPF disease. The inhalation formulation is an aerosol inhalation liquid formulation, an inhalation aerosol, a dry powder inhaler or a soft mist inhaler. The inhalation formulation contains an active drug, and the active drug is any one of apremilast, ibudilast, roflumilast, crisaborole, and difamilast. A preparation process for the inhalation formulation is introduced into a conventional formulation. An active component in a conventional oral formulation is prone to being destroyed in the digestive tract, and has low bioavailability, a liver first pass effect, and a slow onset of action. An inhalation formulation capable of significantly alleviating IPF is prepared. Tests prove that the prepared inhalation formulation can effectively increase the bioavailability, and improve the clinical use effect.

The disclosure relates to methods of treating ocular inflammatory diseases by administering ophthalmic pharmaceutical compositions of roflumilast. Administration of ophthalmic pharmaceutical compositions of roflumilast can result in an improved pharmacokinetic profile relative to existing therapies, including a reduced plasma Cmax and reduced Cmax:C12 trough. As a result, the methods can produce an improved safety and convenience profile relative to existing therapies.

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.

The present invention relates to high concentration ophthalmic pharmaceutical formulations of the phosphodiesterase-4 inhibitor roflumilast suitable for intravitreal administration or other ophthalmic administration to injection sites inside or outside of the eye and orbit. The composition may include from about 2% to about 5% w / v of roflumilast, a viscosity agent, a tension agent, a buffering agent, a surfactant, and water. The pharmaceutical composition is stable, almost free of impurities or free of impurities, and can be injected with minimal force from a No. 27 or No. 30 syringe to achieve therapeutic levels of drugs in the ocular surface, the anterior chamber, the vitreous / posterior chamber, and the tissue associated with the tissue or cavity around the eye.

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.