Roflumilast Formulations with an Improved Pharmacokinetic Profile

    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.

    INHIBITION OF CRYSTAL GROWTH OF ROFLUMILAST
    10.
    发明申请

    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.