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1. 发明申请

US20090302493A1 PROCESS FOR PRODUCING A SOLID DISPERSION OF AN ACTIVE INGREDIENT 审中-公开
标题翻译：生产活性成分固体分散体的方法
公开(公告)号：US20090302493A1
公开(公告)日：2009-12-10
申请号：US12279385
申请日：2007-03-12
申请人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull , Gunther Berndl
发明人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull , Gunther Berndl
IPC分类号： B29C47/60
CPC分类号： A61J3/00 , A61K9/2027 , A61K9/2095 , A61K9/2893 , A61K47/32 , B01F7/0045 , B29C35/02 , B29C48/022 , B29C48/03 , B29C48/04 , B29C48/08 , B29C48/2564 , B29C48/268 , B29C48/2886 , B29C48/29 , B29C48/395 , B29C48/40 , B29C48/402 , B29C48/404 , B29C48/505 , B29C48/52 , B29C48/54 , B29C48/55 , B29C48/56 , B29C48/57 , B29C48/625 , B29C48/65 , B29C48/67 , B29C48/76 , B29C48/83 , B29C48/865 , B29C48/875 , B29C48/906 , B29C48/914 , B29K2105/0005 , B29K2105/0035 , B29K2105/0038 , B29K2105/0064 , B29K2105/16
摘要： A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (R; A), (ii) at least one reverse-flight section (D), and (iii) a discharging section (E), wherein the processing elements defining the reverse-flight section (R; D) comprise at least one reverse-flight element (14) which is based on a screw-type element having a conveying direction being opposite to the general conveying direction of the extruder.
摘要翻译：一种制备活性成分的固体分散体的方法，包括将活性成分和基质形成剂加入到挤出机中并形成均匀的挤出物，其中挤出机包括至少两个旋转轴（2），每个轴 2）承载沿轴向布置的多个处理元件，处理元件限定（i）进料和输送段（R; A），（ii）至少一个反向飞行段（D）和（iii））排出部分（E），其中限定反向飞行部分（R; D）的处理元件包括至少一个反向飞行元件（14），该反向飞行元件基于螺旋型元件，其具有与挤出机的一般输送方向。

2. 发明申请

US20090311414A1 PROCESS FOR PRODUCING A SOLID DISPERSION OF AN ACTIVE INGREDIENT 审中-公开
标题翻译：生产活性成分固体分散体的方法
公开(公告)号：US20090311414A1
公开(公告)日：2009-12-17
申请号：US12279415
申请日：2007-03-12
申请人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull
发明人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull
IPC分类号： B05D3/12 , B29C47/60
CPC分类号： A61J3/00 , A61K9/2027 , A61K9/2095 , A61K9/2893 , A61K47/32 , B01F7/0045 , B29C35/02 , B29C48/022 , B29C48/03 , B29C48/04 , B29C48/08 , B29C48/2564 , B29C48/268 , B29C48/2886 , B29C48/29 , B29C48/395 , B29C48/40 , B29C48/402 , B29C48/404 , B29C48/505 , B29C48/52 , B29C48/54 , B29C48/55 , B29C48/56 , B29C48/57 , B29C48/625 , B29C48/65 , B29C48/67 , B29C48/76 , B29C48/83 , B29C48/865 , B29C48/875 , B29C48/906 , B29C48/914 , B29K2105/0005 , B29K2105/0035 , B29K2105/0038 , B29K2105/0064 , B29K2105/16
摘要： A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element (11, 12, 13) that is derived from a screw type element (FIG. 2).
摘要翻译：一种制备活性成分的固体分散体的方法，包括将活性成分和基质形成剂加入到挤出机中并形成均匀的挤出物，其中挤出机包括至少两个旋转轴（2），每个轴 2）承载多个沿轴向布置的处理元件，处理元件限定（i）进料和输送段（A），（ii）至少一个混合段（B），和（iii）排出段（E），其中限定混合部分（B）的处理元件包括从螺杆型元件（图2）导出的混合元件（11,12,13）。

3. 发明授权

US07014810B2 Method of producing solid shape forms containing an active ingredient 有权
标题翻译：制备含有活性成分的固体形状的方法
公开(公告)号：US07014810B2
公开(公告)日：2006-03-21
申请号：US10149762
申请日：2000-12-15
申请人： Harald Krull , Jörg Rosenberg , Jörg Breitenbach , Jürgen Hofmann , Rainer Klenz , Hans Bührle
发明人： Harald Krull , Jörg Rosenberg , Jörg Breitenbach , Jürgen Hofmann , Rainer Klenz , Hans Bührle
IPC分类号： B29C45/03 , B29C45/72
CPC分类号： B29C45/54 , A61J3/06 , A61K9/2095 , B29C45/542 , B29C2045/466 , B29C2045/545 , B29K2105/0035
摘要： The present invention relates to an apparatus for producing solid active ingredient-containing forms from an active ingredient-containing formulation which comprises at least one polymeric binder. The apparatus according to the invention has at least one extruder 1 for continuous plastication of the formulation and at least two injection units 2 which are provided separate from one another, each of which is connected to the extruder 1, and through which the formulation can be injected into at least one mold 3. In the process according to the invention for producing solid active ingredient-containing forms from an active ingredient-containing formulation which comprises at least one binder, the active ingredient-containing formulation is continuously plasticated, the plasticated formulation is fed into an injection unit 21, and the formulation present in this injection unit 21 is injected into a mold 3, and plasticated formulation is fed into another injection molding unit 22, and the formulation present in the other injection molding unit 22 is injected into the mold 3 or another mold.
摘要翻译：本发明涉及包含至少一种聚合物粘合剂的含活性成分的制剂的含固体活性成分的形式的装置。根据本发明的装置具有至少一个用于制剂的连续塑化的挤出机1和至少两个彼此分离的注射单元2，每个注射单元2彼此连接到挤出机1，并且制剂可以通过该挤出机1 注入至少一个模具3。在根据本发明的用于由含有至少一种粘合剂的含活性成分的制剂生产含固体活性成分的制剂的方法中，含有活性成分的制剂被连续塑化，所述塑化的制剂进料到注射单元2' SUB＆gt; 1，并且将存在于该注射单元2 1中的制剂注射到模具3中，并且将塑化的制剂进料到另一个注射成型单元2 2 / >，并且存在于另一个注射成型单元2 2中的配方被注入到模具3或另一个模具中。

4. 发明申请

US20100247635A1 PHARMACEUTICALLY ACCEPTABLE SOLUBILIZING COMPOSITION AND PHARMACEUTICAL DOSAGE FORM CONTAINING SAME 有权
标题翻译：药物可接受的溶解组合物和含有其的药物剂型
公开(公告)号：US20100247635A1
公开(公告)日：2010-09-30
申请号：US12305870
申请日：2007-07-17
申请人： Jörg Rosenberg , Jörg Breitenbach , Kennan Marsh , Bernd Liepold , Christoph Schmidt , Ute Lander
发明人： Jörg Rosenberg , Jörg Breitenbach , Kennan Marsh , Bernd Liepold , Christoph Schmidt , Ute Lander
IPC分类号： A61K9/48 , A61K47/34 , A61K31/513 , A61P31/18
CPC分类号： A61K47/22 , A61K9/145 , A61K9/146 , A61K9/2013 , A61K9/2027 , A61K9/2095 , A61K9/4833 , A61K9/7007 , A61K31/427 , A61K31/513 , A61K47/14 , A61K47/32 , A61K38/55 , A61K2300/00
摘要： A pharmaceutically acceptable solubilizing composition comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono- and diester is disclosed. The solubilizing composition is useful in the manufacture of a pharmaceutical dosage form which comprises a melt-processed mixture of at least one active ingredient, at least one pharmaceutically acceptable polymer. The active ingredient(s) may be inhibitors of HIV protease. The solubilizing composition enhances the bioavailability of the active ingredient after oral intake.
摘要翻译：公开了一种药学可接受的增溶组合物，其包含（i）至少一种具有聚亚烷基二醇部分的生育酚化合物和（ii）至少一种亚烷基二醇脂肪酸单酯或亚烷基二醇脂肪酸单酯和二酯的混合物。增溶组合物可用于制备药物剂型，其包含至少一种活性成分，至少一种药学上可接受的聚合物的经熔融加工的混合物。活性成分可以是HIV蛋白酶的抑制剂。增溶组合物增加了口服摄入后活性成分的生物利用度。

5. 发明授权

US06423256B1 Process for producing solid dosage forms 有权
标题翻译：生产固体剂型的方法
公开(公告)号：US06423256B1
公开(公告)日：2002-07-23
申请号：US09417070
申请日：1999-10-13
申请人： Stephan Kothrade , Jörg Breitenbach , Harald Krull , Thomas Kessler , Armin Lange , Werner Maier , Ulrich Reinhold
发明人： Stephan Kothrade , Jörg Breitenbach , Harald Krull , Thomas Kessler , Armin Lange , Werner Maier , Ulrich Reinhold
IPC分类号： A61K920
CPC分类号： A61K31/192 , A61K9/2027 , A61K9/2095
摘要： A process for producing solid dosage forms, in which (i) a plastic mixture of at least one pharmacologically acceptable polymeric binder with a K value of more than 75, at least one pharmaceutical active ingredient and, where appropriate, conventional pharmaceutical additives is prepared and (ii) the plastic mixture is shaped to the required dosage form, with step (i) being carried out under conditions of temperature and shear energy input such that the reduction in molecular weight of the polymeric binder, expressed as the difference in the K value, is less than 15 is described.
摘要翻译：一种制备固体剂型的方法，其中（i）至少一种药理学上可接受的聚合物粘合剂与K值大于75的塑料混合物，至少一种药物活性成分以及适当的常规药物添加剂，以及（ii）将塑料混合物成形为所需剂型，步骤（i）在温度和剪切能量输入条件下进行，使得聚合物粘合剂的分子量的降低表示为K值的差异，小于15被描述。

6. 发明授权

US09078921B2 Pharmaceutically acceptable solubilizing composition and pharmaceutical dosage form containing same 有权
标题翻译：药学可接受的增溶组合物和含有它的药物剂型
公开(公告)号：US09078921B2
公开(公告)日：2015-07-14
申请号：US12305870
申请日：2007-07-17
申请人： Jörg Rosenberg , Jörg Breitenbach , Kennan Marsh , Bernd Liepold , Christoph Schmidt , Ute Lander
发明人： Jörg Rosenberg , Jörg Breitenbach , Kennan Marsh , Bernd Liepold , Christoph Schmidt , Ute Lander
IPC分类号： A61P31/18 , A61K47/34 , A61K9/48 , A61K31/513 , A61K47/22 , A61K9/14 , A61K9/20 , A61K31/427 , A61K47/14
CPC分类号： A61K47/22 , A61K9/145 , A61K9/146 , A61K9/2013 , A61K9/2027 , A61K9/2095 , A61K9/4833 , A61K9/7007 , A61K31/427 , A61K31/513 , A61K47/14 , A61K47/32 , A61K38/55 , A61K2300/00
摘要： A pharmaceutically acceptable solubilizing composition comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono- and diester is disclosed. The solubilizing composition is useful in the manufacture of a pharmaceutical dosage form which comprises a melt-processed mixture of at least one active ingredient, at least one pharmaceutically acceptable polymer. The active ingredient(s) may be inhibitors of HIV protease. The solubilizing composition enhances the bioavailability of the active ingredient after oral intake.
摘要翻译：公开了一种药学可接受的增溶组合物，其包含（i）至少一种具有聚亚烷基二醇部分的生育酚化合物和（ii）至少一种亚烷基二醇脂肪酸单酯或亚烷基二醇脂肪酸单酯和二酯的混合物。增溶组合物可用于制备药物剂型，其包含至少一种活性成分，至少一种药学上可接受的聚合物的熔融加工混合物。活性成分可以是HIV蛋白酶的抑制剂。增溶组合物增加了口服摄入后活性成分的生物利用度。

7. 发明申请

US20090220596A1 Composition and Dosage Form Comprising a Solid or Semi-Solid Matrix 审中-公开
标题翻译：包含固体或半固体基质的组合物和剂型
公开(公告)号：US20090220596A1
公开(公告)日：2009-09-03
申请号：US11922609
申请日：2006-06-22
申请人： Jörg Rosenberg , Markus Mäegerlein , Jörg Breitenbach
发明人： Jörg Rosenberg , Markus Mäegerlein , Jörg Breitenbach
IPC分类号： A61K9/20 , A61K9/10
CPC分类号： A61K9/146 , A61K9/1694 , A61K9/2013 , A61K9/2027 , A61K31/4184 , A61K31/5415 , A61K47/22
摘要： A composition which comprises a solid or semi-solid matrix having at least one active ingredient uniformly dispersed therein, the matrix comprising at least one pharmaceutically acceptable matrix-forming agent and a 1,3-bis(lactamyl)-butane compound, in particular 1,3-bis(pyrrolidon-1-yl)-butane. The active ingredient is preferably dispersed in the matrix in a state of a solid solution. The matrix-forming agent is preferably a pharmaceutically acceptable polymer. The composition is useful for the manufacture of pharmaceutical dosage forms.
摘要翻译：一种组合物，其包含固体或半固体基质，其具有均匀分散于其中的至少一种活性成分，所述基质包含至少一种药学上可接受的基质形成剂和1,3-双（内酰胺基） - 丁烷化合物，特别是1 ，3-双（吡咯烷酮-1-基） - 丁烷。活性成分优选以固体状态分散在基质中。基质形成剂优选为药学上可接受的聚合物。该组合物可用于制备药物剂型。

8. 发明申请

US20060269610A1 Method for producing water dispersible dry powders from poorly soluble compounds 审中-公开
标题翻译：从难溶性化合物生产水分散性干粉的方法
公开(公告)号：US20060269610A1
公开(公告)日：2006-11-30
申请号：US10501875
申请日：2003-02-07
申请人： Jörg Rosenberg , Thomas Hantke , Jörg Breitenbach
发明人： Jörg Rosenberg , Thomas Hantke , Jörg Breitenbach
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A23L33/15 , A23V2002/00 , B01J2/00 , A23V2200/224 , A23V2250/314 , A23V2250/54246 , A23V2250/211 , A23V2250/712 , A23V2250/708 , A23V2250/5432 , A23V2250/612
摘要： The invention relates to a method for producing water dispersible dry powders from hardly soluble compounds, whereby a dispersion is provided, containing the poorly soluble compound in a microdispersed form in a dispersion agent. The dispersion of the poorly soluble compound is concentrated by tangential-filtration and the dispersion agent is removed. The invention also relates to preparations based on said water dispersible dry powders.
摘要翻译：本发明涉及一种由难溶化合物制造水分散性干粉的方法，由此提供了一种分散体，其在分散剂中含有微分散形式的难溶性化合物。通过切向过滤浓缩难溶性化合物的分散体，除去分散剂。本发明还涉及基于所述水分散性干粉的制剂。

9. 发明授权

US10653625B2 Production of dosage forms comprising a solid dispersion of a microcrystalline agent 有权
公开(公告)号：US10653625B2
公开(公告)日：2020-05-19
申请号：US11884164
申请日：2006-02-09
申请人： Jörg Rosenberg , Markus Mägerlein , Bernd Liepold , Jörg Breitenbach
发明人： Jörg Rosenberg , Markus Mägerlein , Bernd Liepold , Jörg Breitenbach
IPC分类号： A61K47/30 , A61K9/14
摘要： A method is described for the production of dosage forms, which comprise a solid dispersion of a microcrystalline active substance, in which a thermoplastic polymer with a glass transition temperature Tg of at least 40° C. is melted and an active substance is dissolved homogeneously in the melt; crystallization of the active substance is initiated in the mass obtained; and the mass is cooled. Crystallization of the active substance can be initiated by adding a nonsolvent, seed crystals of the active substance or a derivatization reagent. In addition, crystallization can be initiated by holding the mass for a sufficient length of time at a temperature that is below the temperature at which the active substance is completely soluble in the mass.

10. 发明申请

US20130004578A1 Solid Pharmaceutical Dosage Formulation 审中-公开
标题翻译：固体药物配方
公开(公告)号：US20130004578A1
公开(公告)日：2013-01-03
申请号：US13608482
申请日：2012-09-10
申请人： Jörg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Jörg Breitenbach , Laman Alani , Soumojeet Ghosh
发明人： Jörg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Jörg Breitenbach , Laman Alani , Soumojeet Ghosh
IPC分类号： A61K9/00 , A61P31/18 , A61K31/513
CPC分类号： A61K9/1694 , A61K9/1617 , A61K9/1635 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2031 , A61K9/204 , A61K9/2077 , A61K9/2095 , A61K9/2866 , A61K31/00 , A61K31/426 , A61K31/427 , A61K31/513 , A61K47/32 , A61P31/18 , A61K2300/00
摘要： The present invention provides a pharmaceutical dosage formulation, and more particularly, a pharmaceutical dosage formulation comprising an HIV protease inhibitor.
摘要翻译：本发明提供药物剂量制剂，更具体地，提供包含HIV蛋白酶抑制剂的药物剂型。

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