公开(公告)号：US10105354B1

公开(公告)日：2018-10-23

申请号：US15848505

申请日：2017-12-20

申请人： ARCUTIS, INC.

发明人： David W. Osborne

IPC分类号： A61K31/44 ,  A61K47/10 ,  A61K9/00 ,  A61K9/14 ,  A61K45/06 ,  C09K15/06

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.

公开(公告)号：US11534493B2

公开(公告)日：2022-12-27

申请号：US15712900

申请日：2017-09-22

申请人： ARCUTIS, INC.

发明人： David W. Osborne

IPC分类号： A61K47/10 ,  A61K9/00 ,  A61K9/06 ,  A61K31/44

摘要： 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.

公开(公告)号：US10940142B2

公开(公告)日：2021-03-09

申请号：US16136804

申请日：2018-09-20

申请人： ARCUTIS, INC.

发明人： David W. Osborne

IPC分类号： A61K31/44 ,  C09K15/06 ,  A61K47/10 ,  A61K9/00 ,  A61K9/06 ,  A61K9/14 ,  A61K45/06

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.

公开(公告)号：US20190091333A1

公开(公告)日：2019-03-28

申请号：US15712900

申请日：2017-09-22

申请人： ARCUTIS, INC.

发明人： David W. Osborne

IPC分类号： A61K47/10 ,  A61K31/44

摘要： 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.

公开(公告)号：US20180353490A1

公开(公告)日：2018-12-13

申请号：US15848462

申请日：2017-12-20

申请人： ARCUTIS, INC.

发明人： David W. Osborne

IPC分类号： A61K31/44 ,  A61K47/10 ,  A61K9/14 ,  A61K45/06 ,  C09K15/06 ,  A61K9/00

CPC分类号： A61K31/44 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/145 ,  A61K45/06 ,  A61K47/10 ,  C09K15/06

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.