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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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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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公开(公告)号：US06869617B2
公开(公告)日：2005-03-22
申请号：US09874637
申请日：2001-06-05
IPC分类号： A61K20060101 , 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 , Y10T428/2984 , Y10T428/2985
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 400 nm to 2 microns.
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径为400nm至2微米的颗粒。
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公开(公告)号：US07037528B2
公开(公告)日：2006-05-02
申请号：US09874499
申请日：2001-06-05
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/495 , A61K31/496 , Y10T428/2984 , Y10T428/2985
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 400 nm to 2 microns.
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公开(公告)号：US07193084B2
公开(公告)日：2007-03-20
申请号：US10213352
申请日：2002-08-05
IPC分类号： C07D403/00 , A61K31/497
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 polymorphic form of itraconazole.
摘要翻译： 本发明提供伊曲康唑的多晶型物。
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公开(公告)号：US06607784B2
公开(公告)日：2003-08-19
申请号：US09874799
申请日：2001-06-05
IPC分类号： B01J1302
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K31/495 , A61K31/496 , Y10T428/2984 , Y10T428/2985
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 400 nm to 2 microns.
摘要翻译： 本发明提供了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）将有机化合物 在水混溶的第一溶剂中形成溶液，（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径为400nm至2微米的颗粒。
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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Method for Treating Infectious Organisms Normally Considered to be Resistant to an Antimicrobial Drug 有权治疗通常被认为对抗微生物药物有抵抗力的传染性生物的方法公开(公告)号：US20100086611A1
公开(公告)日：2010-04-08
申请号：US12414484
申请日：2009-03-30
申请人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Tak Wong , James E. Kipp , Mark J. Doty , Christine Rebbeck , Pavlos George Papadopoulos
发明人： Barrett Rabinow , Randy White , Chong-Son Sun , Joseph Chung Tak Wong , James E. Kipp , Mark J. Doty , Christine Rebbeck , Pavlos George Papadopoulos
IPC分类号： A61K9/14 , A61K31/4196 , A61K31/496 , A61K31/4164 , A61K31/505 , A61P31/10
CPC分类号： A61K9/10 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1688 , A61K9/5015 , A61K9/5031 , A61K9/5036 , A61K9/5042 , A61K9/5123 , A61K9/5138 , A61K9/5146 , A61K9/5192 , A61K31/495 , A61K31/496
摘要： The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The composition comprises an aqueous suspension of submicron- to micron-size particles containing the agent coated with at least one surfactant selected from the group consisting of: ionic surfactants, non-ionic surfactants, biologically derived surfactants, and amino acids and their derivatives. The particles have a volume-weighted mean particle size of less than 5 μm as measured by laser diffractometry.
摘要翻译： 本发明涉及抗微生物剂亚微米级微粒的组合物。 更具体地，本发明涉及一种抗微生物剂的组合物，其使得该试剂对通常被认为对该试剂具有抗性的生物有效。 该组合物包含亚微米级至微米级颗粒的含水悬浮液，其含有涂覆有选自以下的至少一种表面活性剂：离子表面活性剂，非离子表面活性剂，生物衍生的表面活性剂，以及氨基酸及其衍生物。 通过激光衍射测量，颗粒具有小于5μm的体积加权平均粒度。
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公开(公告)号：US07067143B2
公开(公告)日：2006-06-27
申请号：US09945374
申请日：2001-08-31
CPC分类号： A61K9/0019 , A61K31/343 , A61K47/26
摘要： A premix parenteral solution for intravenous administration having amiodarone, as an active ingredient, solubilized in a solution of water for injection and about 0.4-12 mg/ml of a non-ionic surfactant to a concentration range of from 0.2 to 6 mg/ml is disclosed. The solution optionally may include an osmotic agent. No dilution of the solution is required before administering to a patient and the sterile packaged solution has an initial pH within the range of from about 2.9 to about 3.2, preferably about 3.1. Additionally, a method for producing an amiodarone solution suitable for intravenous administration is further disclosed.
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公开(公告)号：US06479541B1
公开(公告)日：2002-11-12
申请号：US09539446
申请日：2000-03-30
IPC分类号： A61K31343
CPC分类号： A61K9/0019 , A61K31/34 , A61K47/12
摘要： The present invention provides an amiodarone parenteral solution suitable for intravenous administration without the necessity of dilution. The parenteral solution has an amiodarone concentration from 0.2 to 10 mg/ml and a buffer solution selected from the group consisting of lactate buffer, methanesulfonate buffer, or combinations thereof, the solution having a pH within the range from approximately 2.5-4.5.
摘要翻译： 本发明提供了一种适于静脉内给药而不需要稀释的胺碘酮肠胃外溶液。 肠胃外溶液具有0.2至10mg / ml的胺碘酮浓度和选自乳酸盐缓冲液，甲磺酸盐缓冲液或其组合的缓冲溶液，该溶液的pH值在约2.5-4.5的范围内。
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