INJECTABLE DEPOT FORMULATION COMPRISING CRYSTALS OF ILOPERIDONE
    4.
    发明申请
    INJECTABLE DEPOT FORMULATION COMPRISING CRYSTALS OF ILOPERIDONE 有权
    包含ILOPERIDONE晶体的注射剂配方

    公开(公告)号:US20110212141A1

    公开(公告)日:2011-09-01

    申请号:US13106417

    申请日:2011-05-12

    IPC分类号: A61K9/14 A61K31/454 A61P25/18

    摘要: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.

    摘要翻译: 包含具有结构(I)的晶体的可注射贮库制剂,其中R为(FII)且晶体的X 50值为1至200微米。 含有伊立替康或其代谢物晶体的储备制剂具有以下优点:(i)等离子体中晶体的释放可与晶体尺寸相关; (ii)等离子体中的晶体的吸收可以与晶体的大小相关; (iii)可以通过晶体工程和/或研磨来控制晶体的粒度; 和(iv)晶体在储存时是稳定的,并且对灭菌过程如γ辐射是稳定的。

    Injectable depot formulation comprising crystals of iloperidone
    8.
    发明授权
    Injectable depot formulation comprising crystals of iloperidone 有权
    包含伊潘立酮晶体的可注射贮库制剂

    公开(公告)号:US08293765B2

    公开(公告)日:2012-10-23

    申请号:US13106417

    申请日:2011-05-12

    摘要: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.

    摘要翻译: 包含具有结构(I)的晶体的可注射贮库制剂,其中R为(FII)且晶体的X 50值为1至200微米。 含有伊立替康或其代谢物晶体的储备制剂具有以下优点:(i)等离子体中晶体的释放可与晶体尺寸相关; (ii)等离子体中的晶体的吸收可以与晶体的大小相关; (iii)可以通过晶体工程和/或研磨来控制晶体的粒度; 和(iv)晶体在储存时是稳定的,并且对灭菌过程如γ辐射是稳定的。