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公开(公告)号：US06951656B2
公开(公告)日：2005-10-04
申请号：US09953979
申请日：2001-09-17
IPC分类号： A61K9/10 , A61K9/14 , A61K9/16 , A61K31/495 , A61K31/496 , B01J13/00
CPC分类号： A61K31/495 , A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/496
摘要： The present invention provides a method for preparing submicron sized particles of an organic compound, the solubility of which is greater in a water-miscible first solvent than in a second solvent which is aqueous, the process including the steps of: (i) dissolving the organic compound in the water-miscible first solvent to form a solution, (ii) mixing the solution with the second solvent to define a pre-suspension; and (iii) adding energy to the pre-suspension to form particles having an average effective particle size of less than about 2 μm.
摘要翻译： 本发明提供一种制备有机化合物的亚微米尺寸颗粒的方法，其在水可混溶的第一溶剂中的溶解度大于在水性的第二溶剂中的溶解度，该方法包括以下步骤：（i）将 在水混溶性第一溶剂中形成有机化合物以形成溶液，（ii）将溶液与第二溶剂混合以限定预悬浮液; 和（iii）向预悬浮液中加入能量以形成平均有效粒度小于约2μm的颗粒。
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2.发明申请COMPOSITION OF AND METHOD FOR PREPARING STABLE PARTICLES IN A FROZEN AQUEOUS MATRIX 审中-公开用于在冷冻水质基质中制备稳定颗粒的组合物和方法公开(公告)号：US20060222711A1
公开(公告)日：2006-10-05
申请号：US11425125
申请日：2006-06-19
申请人： James Kipp , Mark Doty , Christine Rebbeck , Sean Brynjelsen , Jamie Konkel
发明人： James Kipp , Mark Doty , Christine Rebbeck , Sean Brynjelsen , Jamie Konkel
IPC分类号： A61K31/573 , A61K31/496 , A61K9/14
CPC分类号： A61K8/044 , A61K8/02 , A61K9/10 , A61K9/145 , A61K9/146 , A61K31/12 , A61K31/4985 , A61K31/58 , A61K2800/92 , A61Q19/00
摘要： The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.
摘要翻译： 本发明公开了悬浮在冷冻水性基质中的药剂或化妆品颗粒形式的水溶性差的药剂或化妆品的稳定悬浮液的组合物及其制备方法。 该组合物长时间稳定，优选6个月或更长时间，适用于肠胃外，口服或非口服途径，如肺（吸入），眼科或局部给药。
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3.发明申请公开(公告)号：US20050013868A1
公开(公告)日：2005-01-20
申请号：US10920578
申请日：2004-08-17
IPC分类号： A61K9/14 , A61K9/19 , A61K9/51 , A61K31/496 , A61K45/00 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/24 , A61K47/28 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/42 , B01J13/04
CPC分类号： A61K9/14 , A61K9/145 , A61K9/5169 , A61K9/5192 , B01J13/04
摘要： The present invention relates to a process for preparing submicron sized nanoparticles of a poorly water soluble compound by lyophilizing a dispersion or microdispersion of a multiphase system having an organic phase and an aqueous phase, the organic phase having the poorly water soluble organic compound therein. The method is preferably used to prepare nanoparticles of a poorly water soluble, pharmaceutically active compound suitable for in vivo delivery, particularly by parenteral routes.
摘要翻译： 本发明涉及通过将具有有机相和水相的多相体系的分散体或微分散体冻干而制备难溶于水的化合物的亚微米尺寸的纳米颗粒的方法，所述有机相在其中具有差的水溶性有机化合物。 该方法优选用于制备适于体内递送的水溶性差的药学活性化合物的纳米颗粒，特别是通过肠胃外途径。
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公开(公告)号：US20060222710A1
公开(公告)日：2006-10-05
申请号：US11425122
申请日：2006-06-19
申请人： James Kipp , Mark Doty , Christine Rebbeck , Sean Brynjelsen , Jamie Konkel
发明人： James Kipp , Mark Doty , Christine Rebbeck , Sean Brynjelsen , Jamie Konkel
IPC分类号： A61K31/573 , A61K31/496 , A61K9/14
CPC分类号： A61K8/044 , A61K8/02 , A61K9/10 , A61K9/145 , A61K9/146 , A61K31/12 , A61K31/4985 , A61K31/58 , A61K2800/92 , A61Q19/00
摘要： The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.
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5.发明申请Preparation of submicron solid particle suspensions by sonication of multiphase systems 审中-公开通过超声处理多相体系制备亚微米固体颗粒悬浮液公开(公告)号：US20050037083A1
公开(公告)日：2005-02-17
申请号：US09964273
申请日：2002-05-10
申请人： Sean Brynjelsen , Shmuel Sternberg , Andy Dunham
发明人： Sean Brynjelsen , Shmuel Sternberg , Andy Dunham
IPC分类号： A61K9/14 , A61K9/19 , A61K9/51 , A61K31/496 , A61K45/00 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/24 , A61K47/28 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/42 , B01J13/02 , B01J13/04
CPC分类号： A61K9/5169 , A61K9/5192
摘要： The present invention provides a method for preparing submicron-sized particles. The method includes the steps of: (1) providing a multiphase system having an organic phase and an aqueous phase, the organic phase having a pharmaceutically effective compound therein; and (2) sonicating the system to evaporate a portion of the organic phase to cause precipitation of the compound in the aqueous phase and having an average effective particle size of less than about 2 m.
摘要翻译： 本发明提供一种制备亚微米尺寸颗粒的方法。 该方法包括以下步骤：（1）提供具有有机相和水相的多相体系，有机相在其中具有药学上有效的化合物; 和（2）超声处理该系统以蒸发有机相的一部分以使化合物在水相中沉淀并具有小于约2μm的平均有效粒度。
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6.发明授权公开(公告)号：US08722091B2
公开(公告)日：2014-05-13
申请号：US10920578
申请日：2004-08-17
IPC分类号： A61K9/14
CPC分类号： A61K9/14 , A61K9/145 , A61K9/5169 , A61K9/5192 , B01J13/04
摘要： The present invention relates to a process for preparing submicron sized nanoparticles of a poorly water soluble compound by lyophilizing a dispersion or microdispersion of a multiphase system having an organic phase and an aqueous phase, the organic phase having the poorly water soluble organic compound therein. The method is preferably used to prepare nanoparticles of a poorly water soluble, pharmaceutically active compound suitable for in vivo delivery, particularly by parenteral routes.
摘要翻译： 本发明涉及通过将具有有机相和水相的多相体系的分散体或微分散体冻干而制备难溶于水的化合物的亚微米尺寸的纳米颗粒的方法，所述有机相在其中具有差的水溶性有机化合物。 该方法优选用于制备适于体内递送的水溶性差的药学活性化合物的纳米颗粒，特别是通过肠胃外途径。
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7.发明授权Compositions of and method for preparing stable particles in a frozen aqueous matrix 有权在冷冻含水基质中制备稳定颗粒的组合物和方法公开(公告)号：US07112340B2
公开(公告)日：2006-09-26
申请号：US10270267
申请日：2002-10-11
IPC分类号： A61K9/14
CPC分类号： A61K8/044 , A61K8/02 , A61K9/10 , A61K9/145 , A61K9/146 , A61K31/12 , A61K31/4985 , A61K31/58 , A61K2800/92 , A61Q19/00
摘要： The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.
摘要翻译： 本发明公开了悬浮在冷冻水性基质中的药剂或化妆品颗粒形式的水溶性差的药剂或化妆品的稳定悬浮液的组合物及其制备方法。 该组合物长时间稳定，优选6个月或更长时间，适用于肠胃外，口服或非口服途径，如肺（吸入），眼科或局部给药。
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8.发明申请Preparation of submicron solid particle suspensions by sonication of multiphase systems 审中-公开通过超声处理多相体系制备亚微米固体颗粒悬浮液公开(公告)号：US20060003012A9
公开(公告)日：2006-01-05
申请号：US09964273
申请日：2001-09-26
申请人： Sean Brynjelsen , Shmuel Sternberg , Andy Dunham
发明人： Sean Brynjelsen , Shmuel Sternberg , Andy Dunham
CPC分类号： A61K9/5169 , A61K9/5192
摘要： The present invention provides a method for preparing submicron-sized particles. The method includes the steps of: (1) providing a multiphase system having an organic phase and an aqueous phase, the organic phase having a pharmaceutically effective compound therein; and (2) sonicating the system to evaporate a portion of the organic phase to cause precipitation of the compound in the aqueous phase and having an average effective particle size of less than about 2 m.
摘要翻译： 本发明提供一种制备亚微米尺寸颗粒的方法。 该方法包括以下步骤：（1）提供具有有机相和水相的多相体系，有机相在其中具有药学上有效的化合物; 和（2）超声处理该系统以蒸发有机相的一部分以使化合物在水相中沉淀并具有小于约2μm的平均有效粒度。
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公开(公告)号：US20050170002A1
公开(公告)日：2005-08-04
申请号：US11052276
申请日：2005-02-07
申请人： James Kipp , Joseph Tak Wong , Mark Doty , Jane Werling , Christine Rebbeck , Sean Brynjelsen
发明人： James Kipp , Joseph Tak Wong , Mark Doty , Jane Werling , Christine Rebbeck , Sean Brynjelsen
IPC分类号： A61K9/10 , A61K9/14 , A61K9/16 , A61K31/495 , A61K31/496 , A61K7/32
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/495 , A61K31/496
摘要： The present invention provides a method for preparing a suspension of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first organic solvent than in a second solvent which is aqueous. The process includes the steps of: (i) dissolving a first quantity of the pharmaceutically-active compound in the water-miscible first organic solvent to form a first solution; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically-active compound; and (iii) seeding the first solution or the second solvent or the pre-suspension.
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公开(公告)号：US06884436B2
公开(公告)日：2005-04-26
申请号：US10021692
申请日：2001-12-12
申请人： James E. Kipp , Joseph Chung Tak Wong , Mark J. Doty , Jane Werling , Christine L. Rebbeck , Sean Brynjelsen
发明人： James E. Kipp , Joseph Chung Tak Wong , Mark J. Doty , Jane Werling , Christine L. Rebbeck , Sean Brynjelsen
IPC分类号： A61K9/10 , A61K9/14 , A61K9/16 , A61K31/495 , A61K31/496 , B01J13/00
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/495 , A61K31/496
摘要： The present invention provides a method for preparing a suspension of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first organic solvent than in a second solvent which is aqueous. The process includes the steps of: (i) dissolving a first quantity of the pharmaceutically-active compound in the water-miscible first organic solvent to form a first solution; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically-active compound; and (iii) seeding the first solution or the second solvent or the pre-suspension.
摘要翻译： 本发明提供了制备药物活性化合物的悬浮液的方法，其在水可混溶的第一有机溶剂中的溶解度大于在水溶液中的溶解度。 该方法包括以下步骤：（i）将第一量的药物活性化合物溶解在水混溶的第一有机溶剂中以形成第一溶液; （ii）将第一溶液与第二溶剂混合以沉淀药物活性化合物; 和（iii）将第一溶液或第二溶剂或预悬浮液接种。
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