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21. 发明授权

US06599528B1 Mechanically stable pharmaceutical presentations form containing liquid or semisolid surface-active substances 有权
标题翻译：包含液体或半固体表面活性物质的机械稳定的药物呈现形式
公开(公告)号：US06599528B1
公开(公告)日：2003-07-29
申请号：US09936349
申请日：2001-09-11
申请人： Jörg Rosenberg , Gunther Berndl , Bernd Liepold , Jörg Breitenbach
发明人： Jörg Rosenberg , Gunther Berndl , Bernd Liepold , Jörg Breitenbach
IPC分类号： A61K948
CPC分类号： A61K9/1617 , A61K9/1635 , A61K9/1694
摘要： The present invention relates to mechanically stable pharmaceutical presentations for oral administration, comprising in addition to one or more active ingredients and at least one melt-processable matrix-forming excipient more than 10 and up to 40% by weight of a surface-active substance with an HLB of from 2 to 18, which is liquid at 20° C. or has a drop point in the range from 20 to 50° C.
摘要翻译：本发明涉及用于口服给药的机械稳定的药物表现，除了一种或多种活性成分和至少一种可熔融加工的基质形成赋形剂之外，还含有超过10重量％至多40重量％的表面活性物质， HLB为2至18，其在20℃下为液体或具有在20至50℃范围内的下降点。

22. 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.

23. 发明申请

US20130118238A1 TEST SOLVENT FOR EVALUATING THE COMPATIBILITY OF BIOLOGICALLY ACTIVE SUBSTANCES AND GRAFT COPOLYMERS 有权
标题翻译：用于评估生物活性物质和共聚物相容性的试验溶液
公开(公告)号：US20130118238A1
公开(公告)日：2013-05-16
申请号：US13578659
申请日：2011-02-15
申请人： Jörg Breitenbach , Bernd Liepold , Jürgen Weis
发明人： Jörg Breitenbach , Bernd Liepold , Jürgen Weis
IPC分类号： G01N33/487
CPC分类号： G01N33/487 , C08F283/06
摘要： A liquid mixture, comprising a) at least one compound selected from polyols, polyol ethers wherein at least one hydroxyl group is unetherified, or polyalkylene ethers wherein at least one terminal hydroxyl group is unetherified, b) 1,3-bis(caprolactam-1-yl) butane, and c) diacetoxybutane mimics the solubility properties of a graft copolymer comprising a poly(alkylene glycol) backbone and a vinyl acetate/N-vinylcaprolactam copolymer grafted onto the backbone. In a method for evaluating the compatibility of a biologically active substance with the graft copolymer i) the biologically active sub-stance is brought into contact with the liquid mixture, and ii) the phase behavior of the test system and/or the solubility of the biologically active substance in the mixture is determined.
摘要翻译：一种液体混合物，其包含a）至少一种选自多元醇的化合物，其中至少一个羟基未醚化的多元醇醚或其中至少一个末端羟基未醚化的聚亚烷基醚，b）1,3-双（己内酰胺-1 - 环烷基）丁烷，和c）二乙酰氧基丁烷模拟包含聚（亚烷基二醇）主链和接枝到主链上的乙酸乙烯酯/ N-乙烯基己内酰胺共聚物的接枝共聚物的溶解性。在用于评价生物活性物质与接枝共聚物的相容性的方法中，i）使生物活性物质与液体混合物接触，和ii）测试体系的相行为和/或溶解度确定混合物中的生物活性物质。

24. 发明授权

US08399015B2 Solid pharmaceutical dosage form 有权
标题翻译：固体药物剂型
公开(公告)号：US08399015B2
公开(公告)日：2013-03-19
申请号：US13240119
申请日：2011-09-22
申请人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Joerg Breitenbach , Laman Alani , Soumojeet Ghosh
发明人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Joerg Breitenbach , Laman Alani , Soumojeet Ghosh
IPC分类号： A61K8/72 , A61K9/20 , A61K9/48 , A61K31/425 , A61K31/505
CPC分类号： A61K47/32 , A61K9/10 , A61K9/1617 , A61K9/1635 , A61K9/2077 , A61K9/2095 , A61K31/427 , A61K31/513 , A61K47/26 , Y10S514/937
摘要： A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
摘要翻译：公开了提供改善的口服生物利用度的固体药物剂型，用于HIV蛋白酶的抑制剂。特别地，剂型包含至少一种HIV蛋白酶抑制剂和至少一种药学上可接受的水溶性聚合物和至少一种药学上可接受的表面活性剂的固体分散体，所述药学上可接受的水溶性聚合物的Tg至少为约50 优选地，药学上可接受的表面活性剂具有约4至约10的HLB值。

25. 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。

26. 发明授权

US08333990B2 Solid pharmaceutical dosage form 有权
公开(公告)号：US08333990B2
公开(公告)日：2012-12-18
申请号：US12880766
申请日：2010-09-13
申请人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Joerg Breitenbach , Laman Alani , Soumojeet Ghosh
发明人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Joerg Breitenbach , Laman Alani , Soumojeet Ghosh
IPC分类号： A61K8/72 , A61K9/20 , A61K9/48 , A61K31/425 , A61K31/505
CPC分类号： A61K47/32 , A61K9/10 , A61K9/1617 , A61K9/1635 , A61K9/2077 , A61K9/2095 , A61K31/427 , A61K31/513 , A61K47/26 , Y10S514/937
摘要： A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

27. 发明申请

US20110182891A1 PHARMACEUTICAL DOSAGE FORM COMPRISING POLYMERIC CARRIER COMPOSITION 审中-公开
标题翻译：包含聚合物载体组合物的药物剂型
公开(公告)号：US20110182891A1
公开(公告)日：2011-07-28
申请号：US13001060
申请日：2009-06-30
申请人： Bernd Liepold , Jörg Breitenbach , Markus Mägerlein , Claudia Packhäuser , Thomas K. Kessler
发明人： Bernd Liepold , Jörg Breitenbach , Markus Mägerlein , Claudia Packhäuser , Thomas K. Kessler
IPC分类号： A61K39/395 , A61K38/43 , A61K31/485 , A61K38/13 , A61K38/28 , A61K31/565 , A61K38/18 , A61K31/566 , A61K38/12 , A61K31/616 , A61K31/43 , A61K33/24 , A61K31/337 , A61P35/00 , A61P29/00 , A61P31/00 , A61P25/04 , A61P5/00
CPC分类号： A61K47/32 , A61K9/2018 , A61K9/2027 , A61K9/2077 , A61K9/2095
摘要： A pharmaceutical dosage form comprises a solid dispersion product of at least one active ingredient dispersed in a polymeric binder composition, the polymeric carrier composition comprising a) a vinylpyrrolidone homopolymer, wherein at least 95% by weight of the vinylpyrrolidone homopolymer has a molecular weight distribution within the range of from 1000 to 13 000; and b) a vinylpyrrolidone copolymer having a weight-average molecular weight of from 5000 to 1 500 000. The dosage form is preferably prepared by a melt extrusion process. The polymeric carrier composition exhibits a high drug dissolution power and allows a reduction of the viscosity of the melt without deteriorating the mechanical properties and storage stability of the dosage form.
摘要翻译：药物剂型包含分散在聚合物粘合剂组合物中的至少一种活性成分的固体分散体产物，所述聚合物载体组合物包含a）乙烯基吡咯烷酮均聚物，其中至少95重量％的乙烯基吡咯烷酮均聚物的分子量分布在范围从1000到13 000; 和b）重均分子量为5000至150000的乙烯基吡咯烷酮共聚物。该剂型优选通过熔融挤出方法制备。聚合物载体组合物表现出高的药物溶解力并且允许熔融物的粘度降低，而不会降低剂型的机械性能和储存稳定性。

28. 发明申请

US20050131054A1 Test system for evaluating the compatibility of biologically active substances with copolymers 有权
标题翻译：用于评估生物活性物质与共聚物的相容性的测试系统
公开(公告)号：US20050131054A1
公开(公告)日：2005-06-16
申请号：US10508483
申请日：2003-03-19
申请人： Joerg Breitenbach , Bernd Liepold
发明人： Joerg Breitenbach , Bernd Liepold
IPC分类号： G01N33/15 , A61K9/14 , A61K47/14 , A61K47/22 , A61K47/32 , C12Q1/00 , A61K31/4025
CPC分类号： A61K9/146 , A61K47/14 , A61K47/22 , Y10T428/31786
摘要： A test solution agent, a test system and a method for evaluating the compatibility of biologically active substances with N-vinylpyrdolidone are disclosed.
摘要翻译：公开了一种测试溶液剂，测试系统和用于评价生物活性物质与N-乙烯基吡啶酮酮的相容性的方法。

29. 发明申请

US20050084529A1 Solid pharmaceutical dosage form 有权
公开(公告)号：US20050084529A1
公开(公告)日：2005-04-21
申请号：US10925442
申请日：2004-08-25
申请人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Jorg Breitenbach , Laman Alani , Soumojeet Ghosh
发明人： Joerg Rosenberg , Ulrich Reinhold , Bernd Liepold , Gunther Berndl , Jorg Breitenbach , Laman Alani , Soumojeet Ghosh
IPC分类号： A61K9/16 , A61K9/20 , A61K31/427 , A61K31/513
CPC分类号： A61K47/32 , A61K9/10 , A61K9/1617 , A61K9/1635 , A61K9/2077 , A61K9/2095 , A61K31/427 , A61K31/513 , A61K47/26 , Y10S514/937
摘要： A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

30. 发明授权

US10463739B2 Solid retard formulations based on solid dispersions 有权
公开(公告)号：US10463739B2
公开(公告)日：2019-11-05
申请号：US13993066
申请日：2011-12-22
申请人： Gunther Berndl , Juergen Weis , Dietrich Granzow , Bernd Liepold , Ute Lander , Ulrich Westedt
发明人： Gunther Berndl , Juergen Weis , Dietrich Granzow , Bernd Liepold , Ute Lander , Ulrich Westedt
IPC分类号： A61K47/34 , A61K9/14 , A61K9/20 , A61K9/00 , A61K31/167 , A61K31/192 , A61K31/216 , A61K47/32
摘要： A formulation comprising a melt-processed solid dispersion product comprising an active agent, a pharmaceutically acceptable thermoplastic polymer of N-vinyl lactams, and a pharmaceutically acceptable polyvinyl alcohol-polyalkylene glycol graft copolymer. A method for producing said formulation.

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