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81. 发明授权

US06444748B1 Preparing aqueous polymer dispersions 失效
标题翻译：制备聚合物水分散体
公开(公告)号：US06444748B1
公开(公告)日：2002-09-03
申请号：US09456514
申请日：1999-12-08
申请人： Maximilian Angel , Karl Kolter , Axel Sanner
发明人： Maximilian Angel , Karl Kolter , Axel Sanner
IPC分类号： C08J2900
CPC分类号： C08F220/14 , C08F2/22 , C08F220/18
摘要： A process for preparing aqueous polymer dispersions by means of a polymerization, conducted in an aqueous system, of at least one free-radically polymerisable ethylenically unsaturated monomer in the presence of a polymerisation initiator, wherein the pH of the aqueous dispersion is adjusted during the preparation process by adding at least two different, basic reagents, at least one of said basic reagents being added in a plurality of stages.
摘要翻译：在聚合引发剂存在下，通过在水系统中进行至少一种可自由基聚合的烯属不饱和单体的聚合制备聚合物水分散体的方法，其中在制备过程中调节水分散体的pH 通过加入至少两种不同的碱性试剂，至少一种所述碱性试剂以多个阶段加入。

82. 发明授权

US6123963A Use of water-soluble or water-dispersible polyurethanes as coatings or binders for pharmaceutical presentations 有权
标题翻译：使用水溶性或水分散性聚氨酯作为药物介绍的涂料或粘合剂
公开(公告)号：US6123963A
公开(公告)日：2000-09-26
申请号：US168098
申请日：1998-10-08
申请人： Son Nguyen Kim , Axel Sanner , Karl Kolter
发明人： Son Nguyen Kim , Axel Sanner , Karl Kolter
IPC分类号： A61K9/20 , A61K9/28 , A61K9/32 , A61K47/30 , A61K9/58
CPC分类号： A61K9/2853 , A61K9/2031
摘要： The use of water-soluble or water-dispersible polyurethanes which consists ofa) 0.1-30% by weight of at least one polyol,b) 20-45% by weight of at least one polyetherpolyol,c) 10-45% by weight of at least one diamine comprising an ionic group,d) 30-50% by weight of at least one polyisocyanate with or withoute) further additives as coatings or binders for pharmaceutical presentations.
摘要翻译：使用水溶性或水分散性聚氨酯，其由以下组成：a）0.1-30重量％的至少一种多元醇，b）20-45重量％的至少一种聚醚多元醇，c）10-45重量％的至少一种包含离子基团的二胺，d）30-50重量％的至少一种多异氰酸酯，其具有或不具有e）另外的添加剂作为用于药物表现的涂层或粘合剂。

83. 发明授权

US6066334A Use of redispersible polymer powders or polymer granules as binders for producing solid pharmaceutical presentations 失效
标题翻译：使用可再分散的聚合物粉末或聚合物颗粒作为制备固体药物表现的粘合剂
公开(公告)号：US6066334A
公开(公告)日：2000-05-23
申请号：US37796
申请日：1998-03-10
申请人： Karl Kolter , Kristin Tiefensee , Katrin Zeitz
发明人： Karl Kolter , Kristin Tiefensee , Katrin Zeitz
IPC分类号： A61K47/04 , A61K9/20 , A61K9/32 , A61K47/12 , A61K47/32 , A61K47/38 , A61K9/14
CPC分类号： A61K9/2027
摘要： Redispersible polymer powders or polymer granules consisting ofa) 10-95% by weight of polyvinyl acetate,b) 5-90% by weight of an N-vinylpyrrolidone-containing polymer,c) 0-20% by weight of another water-soluble or water-swellable substance andd) 0-20% by weight of a water-insoluble dusting agent with or withoute) other additives,are used as binders for producing solid pharmaceutical presentations, where the binder content in the presentation is from 0.5 to 20% by weight.
摘要翻译：可再分散的聚合物粉末或聚合物颗粒，其由a）10-95重量％的聚乙酸乙烯酯，b）5-90重量％的含N-乙烯基吡咯烷酮的聚合物，c）0-20重量％的另一种水溶性或水溶胀性物质和d）0-20重量％的具有或不具有e）其它添加剂的水不溶性除尘剂用作生产固体药物呈现物的粘合剂，其中所述表现中的粘合剂含量为0.5至 20重量％。

84. 发明授权

US6046277A Use of redispersible polymer powders of polymer granules for coating pharmaceutical or agrochemical use forms 失效
标题翻译：使用聚合物颗粒的可再分散聚合物粉末涂覆药物或农用化学品使用形式
公开(公告)号：US6046277A
公开(公告)日：2000-04-04
申请号：US37791
申请日：1998-03-10
申请人： Karl Kolter , Kristin Tiefensee , Reinhold Stadler , Katrin Zeitz
发明人： Karl Kolter , Kristin Tiefensee , Reinhold Stadler , Katrin Zeitz
IPC分类号： A61K47/04 , A01N25/00 , A01N25/10 , A01N25/26 , A61K9/28 , A61K9/32 , A61K9/50 , A61K9/52 , A61K47/12 , A61K47/32 , A61K47/38 , C05G5/00 , C08L35/00 , C08L39/04
CPC分类号： A61K9/284 , A01N25/26 , A61K9/5026 , A61K9/2813 , A61K9/501
摘要： The use of redispersible polymer powders or polymer granules for coating pharmaceutical or agrochemical use forms, consisting ofa) 10-95% by weight of polyvinyl acetate,b) 5-90% by weight of an N-vinylpyrrolidone-containing polymer,c) 0-20% by weight of another water-soluble or water-swellable substance andd) 0-20% by weight of a water-insoluble dusting agent with or withoute) other additives.
摘要翻译：使用可再分散的聚合物粉末或聚合物颗粒来涂覆药物或农业化学品用途形式，由a）10-95重量％的聚乙酸乙烯酯，b）5-90重量％的含N-乙烯基吡咯烷酮的聚合物，c） 0-20重量％的另一种水溶性或水溶胀性物质和d）0-20重量％的具有或不具有e）其它添加剂的水不溶性除尘剂。

85. 发明授权

US5681588A Delayed release microtablet of .beta.-phenylpropiophenone derivatives 失效
标题翻译： β-苯基苯丙酮衍生物的延迟释放微量片
公开(公告)号：US5681588A
公开(公告)日：1997-10-28
申请号：US525749
申请日：1995-10-03
申请人： Karl Kolter , Helmut Fricke , Volker Buehler , Herbert Mueller-Peltzer
发明人： Karl Kolter , Helmut Fricke , Volker Buehler , Herbert Mueller-Peltzer
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/48 , A61K9/52 , A61K31/135 , A61K31/138
CPC分类号： A61K9/2072 , A61K31/135 , A61K31/138 , A61K9/4808
摘要： A cylindrical delayed release tablet with a convex or flat upper side and lower side is provided, along with a method for its production and a gelatin capsule containing 3-200 tablets of the same having identical or different release rates, wherein the tablet if made of .beta.-phenylpropiophenone derivatives of the formula I as active ingredient ##STR1## where R is n-propyl or 1,1-dimethylpropyl, and their pharmacologically acceptable salts, wherein the tablet has a height and diameter that are both, independently of one another, 1-3 mm, the active ingredient content is in the range from 81-99.9% of the weight of the microtablet, (but not taking into account the weight of any coating which is present, the active ingredient density is greater than 1, the release of active ingredient in the USP paddle method at 50 rpm is 80% as a maximum after 3 hours and as a minimum after 24 hours, the release rate is virtually independent of the pressure when compressing the tablets, and the tablet contains no release-delaying ancillary substance but can contain 0.1-5% by weight of a lubricant and 0-18.9% by weight of other conventional ancillary substances.
摘要翻译： PCT No.PCT / EP94 / 00949 Sec。 371 1995年10月3日第 102（e）日期1995年10月3日PCT 1994年3月24日PCT公布。出版物WO94 / 22434 日期：1994年10月3日提供了具有凸形或平坦的上侧和下侧的圆柱形延迟释放片剂及其制备方法和含有相同或不同释放速率的3-200片的明胶胶囊，其中片剂如果由式I的β-苯基苯丙酮衍生物作为活性成分，其中R是正丙基或1,1-二甲基丙基，以及它们的药理学上可接受的盐，其中片剂的高度和直径都是，彼此独立地为1-3mm，活性成分含量在微片的重量的81-99.9％的范围内（但不考虑存在的任何涂层的重量，活性成分密度大于1，USP桨法以50rpm的活性成分在3小时后最大释放80％，24小时后最小释放，释放速度基本上与压片时的压力无关，并且片剂不含释放延迟辅助物质，但可含有0.1-5重量％的润滑剂和0-18.9重量％的其它常规辅助物质。

86. 发明授权

US10406105B2 Pharmaceutical formulation for the production of rapidly disintegrating tablets 有权
公开(公告)号：US10406105B2
公开(公告)日：2019-09-10
申请号：US12663046
申请日：2008-06-03
申请人： Karl Kolter , Michael Schönherr , Silke Gebert , Kathrin Meyer-Böhm , Angelika Maschke
发明人： Karl Kolter , Michael Schönherr , Silke Gebert , Kathrin Meyer-Böhm , Angelika Maschke
IPC分类号： A61K9/16 , A61K9/20 , A61K9/00
摘要： Pharmaceutical formulation in the form of agglomerates comprising A) an excipient content composed of a) 60-97% by weight of sugar or sugar alcohols, b) 1-25% by weight of a disintegrant, c) 1-15% by weight of water-insoluble, film-forming polymers d) 0-15% by weight of water-soluble polymers and e) 0-15% by weight of further pharmaceutically customary excipients the total of the components a) to e) being 100% by weight, and B) at least one active ingredient.

87. 发明授权

US09795576B2 Protective coatings for acidic active ingredients 有权
公开(公告)号：US09795576B2
公开(公告)日：2017-10-24
申请号：US13246324
申请日：2011-09-27
申请人： Karl Kolter , Maximilian Angel
发明人： Karl Kolter , Maximilian Angel
IPC分类号： A61K31/616 , A61K9/00 , A61K31/192 , A61K9/50
CPC分类号： A61K31/192 , A61K9/5073 , A61K31/616
摘要： Dosage forms provided with protective coatings in which a core comprising at least one acidic active ingredient is provided with at least one inner and one outer coating layer, where the outer layer comprises, as component A, a cationic polymer which is an emulsion polymer of N,N-diethylaminoethyl methacrylate and further monomers.

88. 发明授权

US08865250B2 Production of pulverulent coating compositions for stable protective coatings for pharmaceutical dosage forms 有权
标题翻译：生产用于药物剂型的稳定保护性涂料的粉末涂料组合物
公开(公告)号：US08865250B2
公开(公告)日：2014-10-21
申请号：US13406626
申请日：2012-02-28
申请人： Karl Kolter , Maximilian Angel , Bernhard Linner
发明人： Karl Kolter , Maximilian Angel , Bernhard Linner
IPC分类号： A61K9/28 , A61K47/32 , C09D5/03
CPC分类号： A61K47/32 , A61K9/2846 , C09D5/03
摘要： Described are processes for producing pulverulent coating compositions comprising providing an aqueous polymer dispersion comprising i) as component A a polymer obtained by radical polymerization of a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound selected from esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids with C1-C8-alkanols; and spray processing the aqueous polymer dispersion in the presence of a drying gas to provide a powder, wherein the entry temperature of the drying gas into the spraying apparatus is at least 20° C. above the glass transition temperature and is at least 20° C. above the minimum film-forming temperature of the polymer and the exit temperature of the drying gas from the spraying apparatus is kept at 40 to 85° C.
摘要翻译：描述了制备粉状涂料组合物的方法，其包括提供含水聚合物分散体，其包含i）作为组分A的是通过a）N，N-二乙基氨基乙基甲基丙烯酸酯的自由基聚合获得的聚合物，和b）至少一种可自由基聚合的化合物，其选自α ，烯键式不饱和单羧酸和二羧酸与C 1 -C 8 - 链烷醇; 并在干燥气体存在下对聚合物水分散体进行喷雾处理以提供粉末，其中干燥气体进入喷涂装置的入口温度高于玻璃化转变温度至少20℃，并且至少为20℃ 高于聚合物的最低成膜温度和来自喷涂装置的干燥气体的出口温度保持在40至85℃。

89. 发明授权

US08846599B2 Branched polyesters with sulfonate groups 有权
标题翻译：具有磺酸基团的支化聚酯
公开(公告)号：US08846599B2
公开(公告)日：2014-09-30
申请号：US13495444
申请日：2012-06-13
申请人： Monika Haberecht , Frank Rittig , Bernd Bruchmann , Claudia Esper , Roland Ettl , Karl Kolter
发明人： Monika Haberecht , Frank Rittig , Bernd Bruchmann , Claudia Esper , Roland Ettl , Karl Kolter
IPC分类号： C11D1/00 , B08B3/04 , C11D3/37 , C08G63/91 , C08G63/688
CPC分类号： C11D3/378 , C08G63/6888 , C08G63/918
摘要： Branched polyesters with sulfonate groups obtainable by the reaction of the components A, B, optionally C and optionally D to give branched polyesters, where the component A is selected from the group of α,β-olefinically unsaturated dicarboxylic acids, and the component B is selected from the group of tri- or higher-functional alcohols, the optional component C is selected from the group of difunctional alcohols or of difunctional carboxylic acids without α,β-olefinically unsaturated bonds, the optional component D is selected from fatty acids or fatty alcohols, and the subsequent reaction of the resulting branched polyesters with hydrogen sulfite, where the molar amount of hydrogen sulfite is at most 95 mol %, based on the amount of α,β-olefinically unsaturated dicarboxylic acid.
摘要翻译：具有磺酸盐基团的支化聚酯可通过组分A，B，任选的C和任选的D反应获得，得到支链聚酯，其中组分A选自α，β-烯属不饱和二羧酸和组分B 选自三官能或更高官能的醇，任选的组分C选自二官能醇或不具有α，β-烯属不饱和键的双官能羧酸，任选的组分D选自脂肪酸或脂肪醇，以及所得到的支链聚酯与亚硫酸氢盐的随后反应，其中亚硫酸氢盐的摩尔量基于α，α-烯属不饱和二羧酸的量为至多95摩尔％。

90. 发明授权

US08790703B2 Method for producing preparations of substances poorly soluble in water 有权
标题翻译：生产水溶性差的物质的制备方法
公开(公告)号：US08790703B2
公开(公告)日：2014-07-29
申请号：US13262380
申请日：2010-03-30
申请人： Kathrin Meyer-Böhm , Rainer Dobrawa , Stefan Fischer , Karl Kolter
发明人： Kathrin Meyer-Böhm , Rainer Dobrawa , Stefan Fischer , Karl Kolter
IPC分类号： A61K9/14 , C08F283/06 , C08F18/08 , C08F226/06 , C08F226/10 , A61K8/91 , A61K9/20 , A23L1/29 , A23L1/27 , A23L1/30 , A61K47/34 , A61K8/86 , A61K9/16
CPC分类号： A61K9/2095 , A23L5/40 , A23L33/00 , A23L33/10 , A23P10/30 , A61K8/86 , A61K8/91 , A61K9/146 , A61K9/1641 , A61K9/1682 , A61K9/1694 , A61K47/34 , A61Q19/00 , C08F18/08 , C08F226/06 , C08F226/10 , C08F283/06
摘要： The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.
摘要翻译：本发明涉及一种制备少量水溶性物质的制剂的方法，所述微溶物质以无定形嵌入的形式存在于共聚物中，所述共聚物通过i）30至80的混合物的自由基引发聚合而获得重量％的N-乙烯基内酰胺，ii）10-50％重量的乙酸乙烯酯，和iii）10-50％重量的聚醚，条件是组分i），ii）和iii）之和等于 100重量％，其包括在高于易溶性物质的熔点的温度下将微溶物质包埋在共聚物中。

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