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公开(公告)号：US20240000760A1
公开(公告)日：2024-01-04
申请号：US18453674
申请日：2023-08-22
发明人： David Osborne
摘要： An improved a method of 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.
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公开(公告)号：US20230310397A1
公开(公告)日：2023-10-05
申请号：US18176601
申请日：2023-03-01
IPC分类号： A61K31/44 , A61K45/06 , A61K9/00 , A61K47/06 , A61K47/14 , A61K47/24 , A61K47/10 , A61P17/06
CPC分类号： A61K31/44 , A61K9/0014 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/24 , A61P17/06
摘要： 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.
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3.发明公开公开(公告)号：US20230310345A1
公开(公告)日：2023-10-05
申请号：US17887798
申请日：2022-08-15
发明人： David W. OSBORNE , Babak N. TOFIG
CPC分类号： A61K31/08 , A61K9/06 , A61K47/10 , A61K47/548 , A61P31/04
摘要： Self-preserving topical pharmaceutical compositions comprising diethylene glycol monoethyl ether (DEGEE) maintained at an acidic pH. The pH of the formulation can be maintained at a pH of less than 6.3, or alternatively less than 6.0. The topical pharmaceutical compositions disclosed herein are self-preserving and can satisfy European Pharmacopeia Efficacy of Antimicrobial Preservation Criteria A without the addition of a traditional antimicrobial preservative. Certain pharmaceutical composition further comprise an emulsifier blend of cetearyl alcohol, dicetyl phosphate, and ceteth-10 phosphate, which is manufactured by Croda under the tradename Crodafos™ CES.
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公开(公告)号：US20240285595A1
公开(公告)日：2024-08-29
申请号：US18653662
申请日：2024-05-02
发明人： David W. OSBORNE
IPC分类号： A61K31/44 , A61K9/00 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/24 , A61P17/06
CPC分类号： A61K31/44 , A61K9/0014 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/24 , A61P17/06
摘要： 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.
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公开(公告)号：US12042487B2
公开(公告)日：2024-07-23
申请号：US18353870
申请日：2023-07-17
发明人： David W. Osborne
摘要： 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.
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公开(公告)号：US20230414511A1
公开(公告)日：2023-12-28
申请号：US18037316
申请日：2021-11-16
发明人： David W. OSBORNE , Babak N. TOFIG
IPC分类号： A61K9/14 , A61K31/519 , A61K47/24 , A61K9/00 , A61K31/585 , A61K9/107 , A61K47/20
CPC分类号： A61K9/146 , A61K31/519 , A61K47/24 , A61K9/0014 , A61K31/585 , A61K9/1075 , A61K47/20
摘要： Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient and a silicone, such as dimethicone or cyclomethicone, can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.
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公开(公告)号：US20230346690A1
公开(公告)日：2023-11-02
申请号：US18345760
申请日：2023-06-30
发明人： David W. OSBORNE
IPC分类号： A61K9/00 , A61K47/69 , A61P17/06 , A61K9/06 , A61K9/107 , A61K31/122 , A61K31/17 , A61K31/194 , A61K31/366 , A61K31/44 , A61K31/52 , A61K31/5377 , A61K31/573 , A61K31/60 , A61K47/10 , A61K47/14 , A61K47/24
CPC分类号： A61K9/0014 , A61K47/6903 , A61P17/06 , A61K9/06 , A61K9/107 , A61K31/122 , A61K31/17 , A61K31/194 , A61K31/366 , A61K31/44 , A61K31/52 , A61K31/5377 , A61K31/573 , A61K31/60 , A61K47/10 , A61K47/14 , A61K47/24 , A61K45/06
摘要： Decreasing skin penetration lag times will improve the bioavailability of a topically administered roflumilast composition. A shorter skin penetration lag time provides quicker onset of disease relief and more consistent bioavailability as there is less transference to clothing or other people. The skin penetration lag time for roflumilast can be reduced by formulating a roflumilast composition to have a pH between 4.0-6.5 and/or combining roflumilast with an emulsifier blend comprising cetearyl alcohol, dicetyl phosphate and ceteth-10 phosphate.
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公开(公告)号：US11793796B2
公开(公告)日：2023-10-24
申请号：US17102056
申请日：2020-11-23
申请人： ARCUTIS, INC.
发明人： David W. Osborne
摘要： 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 a patient in need of such treatment.
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公开(公告)号：US11707454B2
公开(公告)日：2023-07-25
申请号：US17542072
申请日：2021-12-03
IPC分类号： A61K31/44 , A61K9/00 , A61K31/137 , A61K31/27 , A61K31/343 , A61K31/4174 , A61K31/4418 , A61K31/496 , A61K31/506 , A61K31/60 , A61K33/04 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/24
CPC分类号： A61K31/44 , A61K9/0014 , A61K31/137 , A61K31/27 , A61K31/343 , A61K31/4174 , A61K31/4418 , A61K31/496 , A61K31/506 , A61K31/60 , A61K33/04 , A61K45/06 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/24
摘要： 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.
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公开(公告)号：US11628177B2
公开(公告)日：2023-04-18
申请号：US17527856
申请日：2021-11-16
发明人： David W. Osborne , Babak N. Tofig
IPC分类号： A61K31/585 , A61K9/00 , A61K9/107 , A61K47/34 , A61K31/519
摘要： Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.
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