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公开(公告)号：US20190015398A1
公开(公告)日：2019-01-17
申请号：US16136804
申请日：2018-09-20
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：US09895359B1
公开(公告)日：2018-02-20
申请号：US15616409
申请日：2017-06-07
申请人： ARCUTIS, INC.
发明人： David W. Osborne
CPC分类号： A61K31/44 , A61K9/0014 , A61K9/06 , A61K47/10
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 patient in need of such treatment.
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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：US20210244718A1
公开(公告)日：2021-08-12
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：US10172841B2
公开(公告)日：2019-01-08
申请号：US15848462
申请日：2017-12-20
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：US11129818B2
公开(公告)日：2021-09-28
申请号：US16778845
申请日：2020-01-31
申请人： ARCUTIS, INC.
IPC分类号： A61K31/44 , A61K47/10 , A61K9/00 , A61K47/24 , A61P17/06 , A61K47/06 , A61K47/14 , A61K45/06
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 monoethyl ether, and/or hexylene glycol.
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7.发明申请公开(公告)号：US20200155524A1
公开(公告)日：2020-05-21
申请号：US16563435
申请日：2019-09-06
申请人： ARCUTIS, INC.
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：US09907788B1
公开(公告)日：2018-03-06
申请号：US15676373
申请日：2017-08-14
申请人： ARCUTIS, INC.
发明人： David W. Osborne
CPC分类号： A61K31/44 , A61K9/0014 , A61K9/06 , A61K47/10
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：US09884050B1
公开(公告)日：2018-02-06
申请号：US15676356
申请日：2017-08-14
申请人： ARCUTIS, INC.
发明人： David W. Osborne
CPC分类号： A61K31/44 , A61K9/0014 , A61K9/06 , A61K47/10
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：US20200163944A1
公开(公告)日：2020-05-28
申请号：US16778845
申请日：2020-01-31
申请人： ARCUTIS, INC.
IPC分类号： A61K31/44 , A61K47/10 , A61K47/24 , A61K45/06 , A61K9/00 , A61K47/06 , A61K47/14 , 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 monoethyl ether, and/or hexylene glycol.
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