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公开(公告)号：US20100297194A1
公开(公告)日：2010-11-25
申请号：US12770299
申请日：2010-04-29
申请人： Nathaniel Catron , Michael G. Fickes , Cristina M. Fischer , Rajeev Gokhale , Anthony R. Haight , Katherine Heemstra , David Hill , Martin Knobloch , Drazen Kostelac , Justin S. Lafountaine , Yanxia Li , Bernd Liepold , Kennan Marsh , Jonathan M. Miller , Claudia Packhaeuser , Yeshwant D. Sanzgiri , Eric A. Schmitt , Yi Shi , Norbert Steiger , Ping Tong , Huailiang Wu , Geoff G.Z. Zhang , Deliang Zhou
发明人： Nathaniel Catron , Michael G. Fickes , Cristina M. Fischer , Rajeev Gokhale , Anthony R. Haight , Katherine Heemstra , David Hill , Martin Knobloch , Drazen Kostelac , Justin S. Lafountaine , Yanxia Li , Bernd Liepold , Kennan Marsh , Jonathan M. Miller , Claudia Packhaeuser , Yeshwant D. Sanzgiri , Eric A. Schmitt , Yi Shi , Norbert Steiger , Ping Tong , Huailiang Wu , Geoff G.Z. Zhang , Deliang Zhou
IPC分类号： A61K31/5377 , A61K33/04 , A61K9/14 , A61P35/00
CPC分类号： A61K31/5377 , A61K9/08 , A61K9/10 , A61K9/146 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866
摘要： An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
摘要翻译： 可口服递送的药物组合物包含作为唯一或第一活性成分的本文定义的式I化合物或其药学上可接受的盐，例如ABT-263游离碱或ABT-263双-HCl盐，以游离碱当量 至少约2.5重量％的组合物，在药学上可接受的载体中; 其中所述活性成分是固态形式和/或所述组合物还包含以有效抑制活性成分在其硫醚键的氧化的量分散在载体中的药学上可接受的较重硫族元素抗氧化剂。 该组合物适合于有需要的受试者的口服给药，用于治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）过表达为特征的疾病。
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2.发明申请PHARMACEUTICAL DOSAGE FORM FOR ORAL ADMINISTRATION OF A BCL 2 FAMILY INHIBITOR 有权用于BCL 2家族抑制剂口服给药的药物剂型公开(公告)号：US20100310648A1
公开(公告)日：2010-12-09
申请号：US12796000
申请日：2010-06-08
IPC分类号： A61K31/635 , A61K9/20 , A61K9/48 , A61P35/00
CPC分类号： A61K31/635 , A61K9/0053 , A61K9/146 , A61K9/2013 , A61K9/2027 , A61K9/2095 , A61K9/4833
摘要： The invention relates to a pharmaceutical dosage form which comprises a solid dispersion product comprising N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide or a salt, hydrate or solvate thereof, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer. The invention is further directed to processes for preparing the pharmaceutical dosage form and to use of the dosage form for treating proliferative disorders.
摘要翻译： 本发明涉及药物剂型，其包含固体分散体产物，其包含N-（4-（4 - （（2-（4-氯苯基）-5,5-二甲基-1-环己-1-烯-1-基 ）甲基）哌嗪-1-基）苯甲酰基）-4 - （（1R）-3-（吗啉-4-基）-1 - （（苯基硫烷基）甲基）丙基）氨基）-3 - （（三氟甲基） ）苯磺酰胺或其盐，水合物或溶剂合物，至少一种药学上可接受的聚合物和至少一种药学上可接受的增溶剂。 本发明还涉及制备药物剂型的方法和用于治疗增殖性疾病的剂型的用途。
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公开(公告)号：US09642796B2
公开(公告)日：2017-05-09
申请号：US12796000
申请日：2010-06-08
IPC分类号： A61K9/48 , A61K9/00 , A61K9/14 , A61K31/635
CPC分类号： A61K31/635 , A61K9/0053 , A61K9/146 , A61K9/2013 , A61K9/2027 , A61K9/2095 , A61K9/4833
摘要： The invention relates to a pharmaceutical dosage form which comprises a solid dispersion product comprising N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide or a salt, hydrate or solvate thereof, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer. The invention is further directed to processes for preparing the pharmaceutical dosage form and to use of the dosage form for treating proliferative disorders.
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4.发明授权Preparation of compositions with essentially noncrystalline embedded macrolide antibiotics 有权具有基本上非晶体嵌入的大环内酯类抗生素的组合物的制备公开(公告)号：US08337733B2
公开(公告)日：2012-12-25
申请号：US12673230
申请日：2008-08-14
IPC分类号： B29C47/00
CPC分类号： A61K9/146 , B29C47/40 , B29C47/6056 , B29C47/64
摘要： A description is given of a process for the preparation of a pharmaceutical composition of a macrolide antibiotic in essentially noncrystalline form, in which the macrolide antibiotic, a water-swellable polymer and a proton donor are blended in an extruder in the presence of water and forced through a die, the ratio by weight of the sum of macrolide antibiotic, water-swellable polymer and proton donor to water being at least 1:1. The macrolide antibiotic is preferably clarithromycin and the water-swellable polymer is preferably chosen from crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose and crosslinked polyacrylic acid.
摘要翻译： 描述了制备基本上非结晶形式的大环内酯类抗生素药物组合物的方法，其中大环内酯类抗生素，水溶胀性聚合物和质子供体在水和挤出机的存在下在挤出机中共混 通过模具，大环内酯类抗生素，水溶胀性聚合物和质子供体与水的总量的重量比至少为1:1。 大环内酯类抗生素优选为克拉霉素，水溶胀性聚合物优选选自交联聚乙烯吡咯烷酮，交联羧甲基纤维素钠和交联聚丙烯酸。
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5.发明申请公开(公告)号：US20120001361A1
公开(公告)日：2012-01-05
申请号：US12673230
申请日：2008-08-14
IPC分类号： B29C47/36
CPC分类号： A61K9/146 , B29C47/40 , B29C47/6056 , B29C47/64
摘要： A description is given of a process for the preparation of a pharmaceutical composition of a macrolide antibiotic in essentially noncrystalline form, in which the macrolide antibiotic, a water-swellable polymer and a proton donor are blended in an extruder in the presence of water and forced through a die, the ratio by weight of the sum of macrolide antibiotic, water-swellable polymer and proton donor to water being at least 1:1. The macrolide antibiotic is preferably clarithromycin and the water-swellable polymer is preferably chosen from crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose and crosslinked polyacrylic acid.
摘要翻译： 描述了制备基本上非结晶形式的大环内酯类抗生素药物组合物的方法，其中大环内酯类抗生素，水溶胀性聚合物和质子供体在水和挤出机的存在下在挤出机中共混 通过模具，大环内酯类抗生素，水溶胀性聚合物和质子供体与水的总量的重量比至少为1:1。 大环内酯类抗生素优选为克拉霉素，并且水溶胀性聚合物优选选自交联聚乙烯吡咯烷酮，交联羧甲基纤维素钠和交联聚丙烯酸。
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公开(公告)号：US20100240672A1
公开(公告)日：2010-09-23
申请号：US12447508
申请日：2004-11-08
申请人： Jorg Breitenbach , Norbert Steiger , Harald Hach , Ulrich Westedt , Martin Knobloch , Ralf Altenburger , Nicoletta Loggia , Jörg Ogorka
发明人： Jorg Breitenbach , Norbert Steiger , Harald Hach , Ulrich Westedt , Martin Knobloch , Ralf Altenburger , Nicoletta Loggia , Jörg Ogorka
IPC分类号： A61K31/496 , A61P35/00
CPC分类号： A61K9/2095 , A61K9/2054
摘要： The invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms.
摘要翻译： 本发明提供了一种剂型，其包含（a）药学有效量的伊马替尼或其盐的熔融加工混合物，（b）至少一种聚合物粘合剂，和（c）至少一种药学上可接受的非离子表面活性剂 。 本发明提供具有高药物负荷的伊马替尼剂型，其可以以简单和有效的方式制备，以基本上不依赖于pH的方式释放活性成分的伊马替尼剂型和延长释放的伊马替尼剂型。
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公开(公告)号：US08841303B2
公开(公告)日：2014-09-23
申请号：US12447508
申请日：2007-11-08
申请人： Jörg Breitenbach , Norbert Steiger , Harald Hach , Ulrich Westedt , Martin Knobloch , Ralf Altenburger , Nicoletta Loggia , Jörg Ogorka
发明人： Jörg Breitenbach , Norbert Steiger , Harald Hach , Ulrich Westedt , Martin Knobloch , Ralf Altenburger , Nicoletta Loggia , Jörg Ogorka
IPC分类号： A61K31/497 , A61K9/20
CPC分类号： A61K9/2095 , A61K9/2054
摘要： The invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms.
摘要翻译： 本发明提供了一种剂型，其包含（a）药学有效量的伊马替尼或其盐的熔融加工混合物，（b）至少一种聚合物粘合剂，和（c）至少一种药学上可接受的非离子表面活性剂 。 本发明提供具有高药物负荷的伊马替尼剂型，其可以以简单和有效的方式制备，以基本上不依赖于pH的方式释放活性成分的伊马替尼剂型和延长释放的伊马替尼剂型。
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公开(公告)号：US20090050262A1
公开(公告)日：2009-02-26
申请号：US11884521
申请日：2006-02-17
申请人： Jorg Rosenberg , Norbert Steiger , Harald Hach , Jorg Breitenbach
发明人： Jorg Rosenberg , Norbert Steiger , Harald Hach , Jorg Breitenbach
IPC分类号： B32B37/10
CPC分类号： A61J3/10 , A61J2200/20 , B30B11/16
摘要： Disclosed is a method for producing dosing molds, according to which two separating films (7) are contacted with each other in a defined area, an active substance-containing melt is introduced between the separating films (7) such that a pocket for receiving a portion of the melt is embodied in at least one of the separating films, and the separating films (7) are separated from each other in order to eject the portion. Preferably, a method is disclosed in which the separating films (7) are contacted with each other in the gap of two molding rolls (2, 3) which rotate in opposite directions and are provided with opposite recesses (4, 5) on the surface thereof, and into which the separating films (7) can be pressed when the active substance-containing melt is introduced so as to form pockets. The separating films (7) make it possible to avoid a direct contact between the melt and the rolls (4,5) and thus prevent the melt from adhering to the roll (2, 3). Elastically deformable separating films (7) support the ejection process as a result of the stress thereof being released after leaving the roll gap (2, 3).
摘要翻译： 公开了一种用于生产定量给料模具的方法，根据该方法，两个分离膜（7）在限定的区域中彼此接触，含活性物质的熔体被引入到分离膜（7）之间，使得用于接收 熔体的一部分体现在至少一个分离膜中，并且分离膜（7）彼此分离以便喷射该部分。 优选地，公开了一种方法，其中分离膜（7）在沿相反方向旋转的两个成型辊（2,3）的间隙中彼此接触并且在表面上设置有相对的凹部（4,5） 并且当引入含活性物质的熔体以形成袋时，分离膜（7）可以被压入其中。 分离膜（7）使得可以避免熔体与辊（4,5）之间的直接接触，从而防止熔体粘附到辊（2,3）上。 弹性变形分离膜（7）由于在离开辊间隙（2,3）之后其应力释放而支持喷射过程。
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