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公开(公告)号：US06420473B1
公开(公告)日：2002-07-16
申请号：US09501866
申请日：2000-02-10
申请人： Ramireddy Chittamuru , George Reyes , Thomas P. Farrell , Charles F. Vesey , Dev K. Mehra , Hans-Ulrich Petereit , Klaus Lehmann
发明人： Ramireddy Chittamuru , George Reyes , Thomas P. Farrell , Charles F. Vesey , Dev K. Mehra , Hans-Ulrich Petereit , Klaus Lehmann
IPC分类号： C08J312
CPC分类号： A61K9/2893 , A61K9/2813 , A61K9/2846 , A61K47/02
摘要： A non-toxic, edible, enteric film coating, dry powder composition for use in making an aqueous enteric suspension which may be used in coating pharmaceutical tablets comprises a) an acrylic resin, said resin comprising i) from 20 to 85 percent by weight of at least one alkyl acrylate or alkyl methacrylate moiety, ii) from 80 to 15 percent by weight of at least one vinyl or vinylidene moiety having a carboxylic acid group capable of salt formation, and iii) from 0 to 30 percent by weight of at least one other vinyl or vinylidene moiety copolymerizable with i) and ii), b) an alkalizing agent capable of reacting with the acrylic resin such that, after reaction, 0.1 to 10 mole percent of the acidic groups in 1a-ii) are present in the salt form, and c) a detackifier.
摘要翻译： 可用于制备可用于包衣药物片剂的水性肠溶悬浮液的无毒，可食用的肠溶薄膜包衣干粉组合物包括a）丙烯酸树脂，所述树脂包含i）20至85重量％ 至少一种丙烯酸烷基酯或甲基丙烯酸烷基酯部分，ii）80至15重量％的至少一个具有能够形成盐的羧酸基团的乙烯基或亚乙烯基部分，和iii）至少0至30重量％ 可与i）和ii）共聚的另一个乙烯基或亚乙烯基部分，b）能够与丙烯酸类树脂反应的碱化剂，使得反应后，1a-ii）中的0.1〜10摩尔％的酸性基团存在于 盐形式，和c）防粘剂。
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公开(公告)号：US5292522A
公开(公告)日：1994-03-08
申请号：US998882
申请日：1992-12-28
CPC分类号： A61K9/5073 , A61K9/28 , A61K9/282 , A61K9/2846 , A61K9/5015 , A61K9/5026
摘要： A water insoluble lipophilic emulsifier having a hydrophile-lipophile balance (HLB) of 3.5 to 7, added to an aqueous dispersion containing a polymer comprising acrylic acid, methacrylic acid, their alkyl esters, and/or their alkylaminoalkyl esters, acts as a lubricant and parting agent when the resulting mixture is used for coating pharmaceutical dosage forms and prevents the pharmaceutical dosage forms being coated from sticking to one another and to the walls of the coating apparatus used.
摘要翻译： 将亲水 - 亲油平衡（HLB）为3.5至7的水不溶性亲脂性乳化剂加入到含有丙烯酸，甲基丙烯酸，它们的烷基酯和/或它们的烷基氨基烷基酯的聚合物的水性分散体中，起润滑作用， 当所得到的混合物用于涂覆药物剂型并防止药物剂型被涂覆时彼此粘附和使用的涂覆装置的壁分离剂。
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公开(公告)号：US06306428B1
公开(公告)日：2001-10-23
申请号：US09058951
申请日：1998-04-13
IPC分类号： A61K900
CPC分类号： A61K9/2095 , A61K9/2072 , A61K9/2086 , A61K9/7007
摘要： A time-release laminar pharmaceutical composition, comprised of rolled or folded layers of a polymer film, that contain a pharmaceutically active substance, in which the outer surface area of the polymer film which contains the active substance, and which is accessible to the digestive juices, amounts to at most 25% of the entire surface area in the rolled or folded state, and the rolled or folded layers adhere to one another in such a way that the laminar form of medication maintains its rolled or folded form for a period of at least one hour in the release test according to USP 23, Method A, apparatus 2, at 37° C. and 50 rpm, in artificial gastric juice, and at least 30% of the active substance contained in it is released in the rolled or folded state.
摘要翻译： 包含聚合物膜的卷曲或折叠层的时间释放层状药物组合物，其含有药物活性物质，其中含有活性物质的聚合物膜的外表面积并且可被消化液接触 相当于轧制或折叠状态下整个表面积的至多25％，并且卷起或折叠的层彼此粘合，使得层状形式的药物保持其卷曲或折叠形式一段时间 根据USP 23，方法A，装置2在37℃和50rpm，在人造胃液中的释放试验中至少1小时，其中含有的至少30％的活性物质被释放在轧制或 折叠状态。
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4.发明授权
公开(公告)号：US5730999A
公开(公告)日：1998-03-24
申请号：US650025
申请日：1996-05-17
CPC分类号： A61K9/7061 , A61L15/44 , A61L15/58 , A61L2300/40 , A61L2300/418 , A61L2300/434 , A61L2300/602
摘要： A dermal therapeutic system which exhibits a prolonged release of a drug comprising at least one pharmaceutical agent combined with poly(meth)acrylates in the form of at least one layer of the therapeutic system, the poly(meth)acrylates being a mixture, which is produced from a melt, comprising (1) at least one (meth)acrylic polymer containing functional groups and (2) at least one (meth)acrylic polymer which regulates the flow behavior of the poly(meth)acrylate mixture and which contains no functional groups or only insignificant amounts of functional groups.
摘要翻译： 显示药物延长释放的真皮治疗系统，其包含至少一种药物剂，其与至少一层治疗系统形式的聚（甲基）丙烯酸酯组合，所述聚（甲基）丙烯酸酯是混合物，其为 由（1）至少一种含有官能团的（甲基）丙烯酸聚合物和（2）调节聚（甲基）丙烯酸酯混合物的流动行为的至少一种（甲基）丙烯酸类聚合物，其不含功能性 组或仅有微量的官能团。
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公开(公告)号：US5342646A
公开(公告)日：1994-08-30
申请号：US979425
申请日：1992-11-19
CPC分类号： G01N33/545 , C07K17/08 , C12N11/08
摘要： What is disclosed is a method for preparing carrier systems, adaptable to the covalent bonding thereto of biologically active materials, consisting of a known solid support material having a surface coated with a polymer containing functional groups suitable for covalent bonding, by coating the support material with a film-forming polymer dispersion and a non-film-forming polymer dispersion, suitably in admixture, at least one of the two polymer dispersions containing a polymer having functional groups suitable for covalent bonding with a biologically active material.
摘要翻译： 公开的是一种制备载体系统的方法，其适用于生物活性材料的共价键合，其由已知的固体支持材料组成，所述固体支持材料具有涂覆有包含适于共价键合的官能团的聚合物的表面，通过用 一种成膜聚合物分散体和一种非成膜聚合物分散体，适当地混合两种聚合物分散体中的至少一种，其含有具有适于与生物活性材料共价键合的官能团的聚合物。
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公开(公告)号：US09107451B2
公开(公告)日：2015-08-18
申请号：US12845994
申请日：2010-07-29
CPC分类号： A23P1/04 , A23P10/30 , A61K9/4891 , A61K47/32
摘要： A coating composition for the enteric coating of capsule halves made of water-soluble or water-swellable polymer material in a dipping process is provided. The composition is an aqueous dispersion or solution, containing a polymer mixture of at least one first (meth)acrylate copolymer, which is enteric, and at least one further (meth)acrylate copolymer, which is enteric or water-insoluble, and also auxiliaries which influence the viscosity of the dispersion and the elasticity of the dried polymer film. The solids content of the dispersion or solution is more than 25% by weight and the viscosity is 150 to 1500 mPa·s and a dried film produced from the dispersion or solution has an elongation at break of at least 200%. Also provided is a capsule composed of two capsule halves coated with the dispersion or solution in a dipping process does. The enteric capsule does not dissolve in 0.1 N HCl at pH 1.2 after two hours, but completely dissolves in buffer at pH 6.8 in less than 30 minutes. A method to prepare enteric coated capsule halves is also provided.
摘要翻译： 提供了一种用于在浸渍过程中由水溶性或水溶胀性聚合物材料制成的胶囊半部的肠溶衣涂料组合物。 该组合物是含有至少一种肠溶性的至少一种第一（甲基）丙烯酸酯共聚物和至少一种其它（甲基）丙烯酸酯共聚物的聚合物混合物的水性分散体或溶液，其为肠溶或水不溶性的，以及辅助剂 这影响了分散体的粘度和干燥的聚合物膜的弹性。 分散体或溶液的固体成分大于25重量％，粘度为150〜1500mPa·s，由分散液或溶液产生的干燥膜的断裂伸长率为200％以上。 还提供了由在浸渍过程中涂覆有分散体或溶液的两个胶囊半部组成的胶囊。 肠溶胶囊在pH2.2后2小时内不溶于0.1N HCl，但在不到30分钟内完全溶于pH 6.8的缓冲液中。 还提供了制备肠溶衣胶囊半部的方法。
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公开(公告)号：US08431157B2
公开(公告)日：2013-04-30
申请号：US11815632
申请日：2005-12-15
CPC分类号： C08F220/18 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a partly neutralized anionic (meth)acrylate copolymer consisting of radically polymerized units containing 25-95% by weight (meth)acrylic acid C1 to C4 alkylesters and 5-75% by weight (meth)acrylate monomer with an anionic group, wherein 0.1 to 25% contained anionic groups are neutralized by a base. Said invention is characterized in that said base is embodied in the form of an cationic organic base whose molecular weight is greater than 150. A medical form containing said partly neutralized anionic (meth)acrylate copolymer and the use of said partly neutralized anionic (meth)acrylate copolymer for producing a medical form rapidly releasing an active substance having a determined pH value are also disclosed.
摘要翻译： 本发明涉及一种部分中和的阴离子（甲基）丙烯酸酯共聚物，它由含25-95％（重量）（甲基）丙烯酸C1至C4烷基酯和5-75％（重量）（甲基）丙烯酸阴离子基团单体的自由基聚合单元组成 ，其中0.1〜25％的阴离子基团被碱中和。 所述发明的特征在于所述碱以分子量大于150的阳离子有机碱的形式实施。含有所述部分中和的阴离子（甲基）丙烯酸酯共聚物的医用形式以及所述部分中和的阴离子（甲基）丙烯酸酯共聚物的用途， 丙烯酸酯共聚物，用于制备快速释放具有确定的pH值的活性物质的医用形式。
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公开(公告)号：US08343542B2
公开(公告)日：2013-01-01
申请号：US10542283
申请日：2003-11-21
CPC分类号： A61J3/10 , A61K9/0056 , A61K9/146 , A61K9/1647 , A61K9/2054 , A61K31/192
摘要： The invention relates to a method for producing an oral form of administration which decomposes immediately and releases active ingredients in the mouth. According to said method, (a) an anionic pharmaceutical active ingredient is intensively mixed with (b) a copolymer consisting of radically polymerized C1-C4 esters of the acrylic acid or methacrylic acid and other (meth)acrylate monomers containing functional tertiary amino groups, and (c) between 5 and 50 wt. %, in relation to (b), of a C12-C22 carboxylic acid in the melted mass; the mixture is solidified and ground to form a powder containing active ingredients having an average particle size of 200 μm or less; and the powder is encapsulated in a water-soluble matrix consisting of pharmaceutically standard adjuvants, on the condition that no more than 3 wt. %, in relation to the copolymer, of emulsifiers with an HLB value of at least 14 must be contained therein. The invention also relates to the powder containing active ingredients and the uses of the same.
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9.发明申请PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT 有权通过分散剂将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法公开(公告)号：US20120208832A1
公开(公告)日：2012-08-16
申请号：US13504527
申请日：2009-11-16
IPC分类号： A61K47/32 , C08K5/11 , C08K5/1535 , A61P11/00 , C08K5/41 , C09D105/00 , A61K31/522 , C08L5/00 , C08K5/06
CPC分类号： C08J3/03 , A61K9/284 , A61K9/5026 , A61K9/5089 , C08J3/05 , C08J2333/14
摘要： The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50° C.
摘要翻译： 本发明提供了一种将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法，其中制备含有（a）（甲基）丙烯酸酯共聚物的组分的水性分散体，该组分由自由基聚合的甲基丙烯酸甲酯，丙烯酸乙酯和 以甲基丙烯酸2-三甲基铵乙酯为盐，粉末形式为固体形式，或以颗粒形式存在，（b）按（b）所示的分散剂的（甲基）丙烯酸酯共聚物（a）计算的至多50重量％ ）i）与乳化剂组合的增塑剂和/或（b）ii）具有官能团的具有6至18个碳原子的药学上可接受的碳水化合物和（c）通过将组分（a），（b）和（c） 得到在将固体（甲基）丙烯酸酯共聚物转化成分散形式时成为水分散体的悬浮液，其特征在于，通过存在分散体将（甲基）丙烯酸酯共聚物转化为分散形式 g试剂在低于50℃的温度下
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10.发明申请POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A DICARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID 审中-公开包含共聚物，二羧酸和脂肪单羧酸的粉末或成粒组合物公开(公告)号：US20120071565A1
公开(公告)日：2012-03-22
申请号：US13322159
申请日：2009-07-30
摘要： A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C1- to C4-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).
摘要翻译： 一种粉状或粒状组合物，其含有：（a）以聚合形式含有丙烯酸或甲基丙烯酸的C 1至C 4烷基酯和在烷基中含有叔氨基的（甲基）丙烯酸烷基酯单体的共聚物; （b）相对于（a）碳原子数为3〜10的二羧酸为0.5〜10重量％ 和（c）基于（a）具有8至18个碳原子的脂肪一元羧酸的5至20重量％，其中所述组合物含有至少30重量％的（a），（b）和（c ）。
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