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公开(公告)号：US08227488B2
公开(公告)日：2012-07-24
申请号：US13401310
申请日：2012-02-21
IPC分类号： A01N43/00 , A01N43/40 , A61K31/553 , A61K31/554 , A61K31/445 , C08J9/28 , C07D211/22 , C07D261/20
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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.
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公开(公告)号：US20050250813A1
公开(公告)日：2005-11-10
申请号：US10521064
申请日：2003-07-14
IPC分类号： C07D413/04 , A61K9/10 , A61K31/454 , A61K47/10 , A61K47/14 , A61K47/24 , A61K47/26 , A61K47/34 , A61K47/36 , A61K47/38 , A61P25/28
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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 metabolite 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。 含有伊洛哌啶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。
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公开(公告)号：US08293765B2
公开(公告)日：2012-10-23
申请号：US13106417
申请日：2011-05-12
IPC分类号： A01N43/00 , A01N43/40 , A61K31/553 , A61K31/554 , A61K31/445 , C08J9/28 , C07D211/22 , C07D261/20
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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。
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公开(公告)号：US20130012542A1
公开(公告)日：2013-01-10
申请号：US13618753
申请日：2012-09-14
IPC分类号： C07D413/04 , A61P25/18 , A61K31/454
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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.
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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
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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。
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公开(公告)号：US08614232B2
公开(公告)日：2013-12-24
申请号：US13618753
申请日：2012-09-14
IPC分类号： A61K8/02 , C12Q1/68 , C12Q1/02 , A01N43/00 , A61K31/553 , A61K31/554 , A01N43/40 , A61K31/445
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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。
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公开(公告)号：US20120156264A1
公开(公告)日：2012-06-21
申请号：US13401310
申请日：2012-02-21
IPC分类号： A61K31/4439 , A61P25/18 , A61K9/00
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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。
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公开(公告)号：US20090099232A1
公开(公告)日：2009-04-16
申请号：US12254925
申请日：2008-10-21
IPC分类号： A61K31/454
CPC分类号： A61K31/454 , A61K9/0019 , A61K47/10 , A61K47/26 , A61K47/38
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。
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公开(公告)号：US08124795B2
公开(公告)日：2012-02-28
申请号：US13198022
申请日：2011-08-04
申请人： Sabine Pfeffer , Dierk Wieckhusen
发明人： Sabine Pfeffer , Dierk Wieckhusen
IPC分类号： C07D307/78
CPC分类号： C07D307/88 , A61K9/14 , A61K9/2866
摘要： A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.
摘要翻译： 提供了一种改变针状药物晶体习性的方法，通过这种方法获得的晶体，以及特定的霉酚酸或霉酚酸钠的晶型或改性物，以及包含晶体，治疗方法及其用途的药物组合物。
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公开(公告)号：US20110288313A1
公开(公告)日：2011-11-24
申请号：US13198022
申请日：2011-08-04
申请人： Sabine Pfeffer , Dierk Wieckhusen
发明人： Sabine Pfeffer , Dierk Wieckhusen
IPC分类号： C07D307/88
CPC分类号： C07D307/88 , A61K9/14 , A61K9/2866
摘要： A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.
摘要翻译： 提供了一种改变针状药物晶体习性的方法，通过这种方法获得的晶体，以及特定的霉酚酸或霉酚酸钠的晶型或改性物，以及包含晶体，治疗方法及其用途的药物组合物。
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