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公开(公告)号：US20110033530A1
公开(公告)日：2011-02-10
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，由分散液或溶液制得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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12.发明授权Use of a partially neutralized, anionic (meth) acrylate copolymer as a coating for the production of a medicament pharmaceutical form releasing active substance at reduced pH values 有权使用部分中和的阴离子（甲基）丙烯酸酯共聚物作为涂层，用于制备在降低的pH值下释放活性物质的药物形式公开(公告)号：US07932258B2
公开(公告)日：2011-04-26
申请号：US11994440
申请日：2006-04-05
IPC分类号： A61K31/522
CPC分类号： A61K9/5026 , A61K9/2081 , A61K9/2846
摘要： The invention relates to the use of a partially neutralized, anionic (meth)acrylate copolymer comprising radically polymerized units of 25 to 95 percent by weight of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 75 percent by weight of (meth)acrylate monomers with an anionic group, at least 4 percent of which are neutralized by means of a base, for producing a medicament that is provided with an active substance-containing core and is coated with the partially neutralized, anionic (meth)acrylate copolymer. The medicament releases at least 30 percent of the active substance contained therein in 30 minutes at a pH at which the active substance is sufficiently soluble and stable and at which the corresponding medicament that is coated with the non-neutralized anionic (meth)acrylate polymer releases less than 10 percent of the active substance contained therein.
摘要翻译： 本发明涉及部分中和的阴离子（甲基）丙烯酸酯共聚物的用途，其包括25至95重量％的丙烯酸或甲基丙烯酸的C 1至C 4烷基酯和5至75重量％的（甲基）丙烯酸酯的自由基聚合单元， 丙烯酸酯单体，其中至少4％通过碱中和，用于生产具有含活性物质的芯并涂覆有部分中和的阴离子（甲基）丙烯酸酯共聚物的药物。 在活性物质具有足够的可溶性和稳定性的pH下，药物在30分钟内释放至少30％的活性物质，其中涂覆有未中和的阴离子（甲基）丙烯酸酯聚合物的相应药物释放 少于其中含有的活性物质的10％。
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13.发明申请Multilayer dosage form comprising a matrix that influences release of a modulatory substance 审中-公开包含影响调节物质释放的基质的多层剂型公开(公告)号：US20070042045A1
公开(公告)日：2007-02-22
申请号：US10573019
申请日：2004-09-15
IPC分类号： A61K9/24
CPC分类号： A61K9/5078 , A61K9/5026
摘要： The invention relates to a multilayer pharmaceutical form for controlled active ingredient release, essentially comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth)acrylate copolymers composed of 98 to 85 C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 15% by weight of methacrylate monomers with a quaternary ammonium group in the alkyl radical, and, where appropriate, further water-insoluble pharmaceutically usable polymers, where the layers may additionally and in a manner known per se comprise pharmaceutically usual excipients.
摘要翻译： 本发明涉及用于受控活性成分释放的多层药物形式，其基本上包括a）任选的中性核心（非矫正剂），b）内部控制层，其包含具有调节作用的物质，其嵌入影响递送的基质中 的调节物质，并且其包含药学上可用的聚合物，蜡，树脂和/或蛋白质，并且在适当的情况下为活性成分，c）活性成分层，其包含活性药物成分和适当时具有调节作用的物质，d ）外部控制层，其包含至少60重量％的由98至85℃1至C 4的至少一种或多种（甲基）丙烯酸酯共聚物的混合物， （甲基）丙烯酸的烷基酯和2至15重量％的在烷基中具有季铵基团的甲基丙烯酸酯单体，以及在适当情况下进一步的水不溶性药学上可接受的聚 其中层可以另外地以本身已知的方式包含药学上通常的赋形剂。
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公开(公告)号：US06632454B2
公开(公告)日：2003-10-14
申请号：US09926567
申请日：2001-11-19
IPC分类号： A61K958
CPC分类号： A61K9/5073 , A61K9/2846 , A61K9/2886 , A61K9/5026
摘要： The invention relates to the use of a multilayer pharmaceutical product that substantially comprises a) a core containing a pharmaceutically active substance, b) an inner coating consisting of a copolymer or a mixture of copolymers that are composed of 85 to 98 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 15 to 2 wt.- % of (meth)acrylate monomers with a quaternary ammonium group in the alkyl group, and c) an outer coating consisting of a copolymer that is composed of 75 to 95 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 5 to 25 wt.- % of (meth)acrylate monomers with an anionic group in the alkyl group. The inventive product is used for producing a pharmaceutical product that releases the active substance contained therein according to the USP release test, at pH 1.2 during 2 hours and subsequent rebuffering to pH 7.0, by less than 5% after 2.0 hours after start of the test and by 30 to 80% after eight hours after start of the test.
摘要翻译： 本发明涉及多层药物产品的应用，其基本上包括a）含有药物活性物质的核心，b）由共聚物或共聚物混合物组成的内涂层，其由85-98wt。％的 丙烯酸或甲基丙烯酸的自由基聚合的C1-C4烷基酯和在烷基中具有季铵基团的15至2重量％的（甲基）丙烯酸酯单体，和c）由共聚物组成的外涂层， 75至95重量％的丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯和5至25重量％的在（甲基）丙烯酸烷基酯中具有阴离子基团的（甲基）丙烯酸酯单体。 本发明产品用于生产一种药物产品，根据USP的释放试验，在pH2.2的时间内释放其中所含的活性物质，并在试验开始后的2.0小时内，随后的反渗透至pH 7.0，小于5％ 并且在开始测试后八小时后，再增加30到80％
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15.发明授权Multi-particulate form of medicament, comprising at least two differently coated forms of pellet 有权多颗粒形式的药物，包含至少两种不同的包衣形式的丸剂公开(公告)号：US07438929B2
公开(公告)日：2008-10-21
申请号：US10949323
申请日：2004-09-27
CPC分类号： A61K31/58 , A61K9/2081 , A61K9/5026 , A61K9/5073 , A61K9/5084 , A61K31/573 , A61K31/606 , A61K31/635
摘要： The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
摘要翻译： 本发明涉及适于在小肠和大肠中均匀释放活性药物成分的多颗粒药物形式，其包含至少两种形式的颗粒A和B，其包含芯中的活性药物成分并具有不同的聚合物 确定在不同pH值下释放活性成分的涂层，其特征在于，颗粒形式A具有能够连续释放活性成分的内部聚合物涂层，并且具有快速溶解在约pH 5.5以上的外部肠溶衣，以及 颗粒形式B具有聚合物涂层，其在USP释放试验中在6小时内在pH 6.8下释放少于20％的活性成分，并在6小时内在pH 7.2下释放超过50％的活性成分。 本发明还涉及生产多颗粒药物形式的方法以及用于制备药物形式的颗粒形式A和B的用途。
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16.发明授权公开(公告)号：US06897205B2
公开(公告)日：2005-05-24
申请号：US10239209
申请日：2001-03-09
IPC分类号： A61K9/16 , A61K9/20 , A61K9/26 , A61K9/50 , A61K9/54 , A61K9/58 , A61K9/62 , A61K31/573 , A61K31/58 , A61K31/606 , A61K31/635 , A61K47/32 , A61K47/36 , A61K47/38 , A61P1/00 , A61K31/60 , A61K31/54 , A61K31/56 , A61K38/00
CPC分类号： A61K31/58 , A61K9/2081 , A61K9/5026 , A61K9/5073 , A61K9/5084 , A61K31/573 , A61K31/606 , A61K31/635
摘要： The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
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公开(公告)号：US06878387B1
公开(公告)日：2005-04-12
申请号：US09787438
申请日：1999-09-28
IPC分类号： A61K47/32 , A61K9/22 , A61K9/32 , A61K9/50 , A61K9/52 , A61K9/58 , A61K9/64 , A61K31/522 , A61K47/12 , A61P11/06 , C08F220/18 , C08L33/04 , A61K9/14 , A61K9/16 , A61K9/46 , A61K9/48
CPC分类号： A61K9/5078 , A61K9/5026 , A61K31/522
摘要： The invention relates to a pharmaceutical preparation consisting of: (a) a core containing an active substance, optionally an excipient and common pharmaceutical additives in addition to the salt of an inorganic acid whose proportion in the weight of the core ranges from 2.5 to 97% by weight and (b) and outer film coating consisting of one or more (meth)acrylate copolymers and optionally common pharmaceutical adjuvants, wherein 40 to 100% by weight of the (meth)acrylate copolymers consist of 93 to 98% by weight of radically polymerized C1- to C4-alkylesters of acrylic or methacrylic acid and 7 to 2% by weight of (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical and that may be optionally present in a mixture consisting of 1 to 60% by weight of one or more additional (meth)acrylate copolymers different from the above-mentioned (meth)acrylate copolymers, consisting of 85 to 100% by weight of a radically polymerized C1- to C4-alkylesters of acrylic orethacrylic acid and optionally and optionally up to 15% by weight of additional (meth)acrylate monomers with basic groups or acid groups in the alkyl radical.
摘要翻译： 本发明涉及一种药物制剂，其包含：（a）含有活性物质的核心，任选的赋形剂和常见的药用添加剂，除了无机酸的盐，其核心重量的比例为2.5至97％ （b）和由一种或多种（甲基）丙烯酸酯共聚物和任选的普通药用佐剂组成的外膜包衣，其中40至100重量％的（甲基）丙烯酸酯共聚物由93至98重量％ 聚合丙烯酸或甲基丙烯酸的C 1至C 4 - 烷基酯和7至2重量％的在烷基中具有季铵基团的（甲基）丙烯酸酯单体，并且其可以任选地存在于由1至60％ 一种或多种与上述（甲基）丙烯酸酯共聚物不同的另外的（甲基）丙烯酸酯共聚物的重量，其由85至100重量％的丙烯酸类聚丙烯酸酯的自由基聚合的C 1 -C 4烷基酯 酸和任选地和任选地至多15重量％的在烷基中具有碱性基团或酸基团的另外的（甲基）丙烯酸酯单体。
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18.发明申请Multi-particulate form of medicament, comprising at least two differently coated forms of pellet 有权多颗粒形式的药物，包含至少两种不同的包衣形式的丸剂公开(公告)号：US20050053660A1
公开(公告)日：2005-03-10
申请号：US10949323
申请日：2004-09-27
IPC分类号： A61K9/16 , A61K9/20 , A61K9/26 , A61K9/50 , A61K9/54 , A61K9/58 , A61K9/62 , A61K31/573 , A61K31/58 , A61K31/606 , A61K31/635 , A61K47/32 , A61K47/36 , A61K47/38 , A61P1/00
CPC分类号： A61K31/58 , A61K9/2081 , A61K9/5026 , A61K9/5073 , A61K9/5084 , A61K31/573 , A61K31/606 , A61K31/635
摘要： The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
摘要翻译： 本发明涉及适于在小肠和大肠中均匀释放活性药物成分的多颗粒药物形式，其包含至少两种形式的颗粒A和B，其包含芯中的活性药物成分并具有不同的聚合物 确定在不同pH值下释放活性成分的涂层，其特征在于，颗粒形式A具有能够连续释放活性成分的内部聚合物涂层，并且具有快速溶解在约pH 5.5以上的外部肠溶衣，以及 颗粒形式B具有聚合物涂层，其在USP释放试验中在6小时内在pH 6.8下释放少于20％的活性成分，并在6小时内在pH 7.2下释放超过50％的活性成分。 本发明还涉及生产多颗粒药物形式的方法以及用于制备药物形式的颗粒形式A和B的用途。
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19.发明申请Multilayer dosage forms, which contain active substances and which comprise a neutral core, and an inner and outer coating consisting of methacrylate copolymers and methacrylate monomers 审中-公开包含活性物质并且包含中性核心的多层剂型，以及由甲基丙烯酸酯共聚物和甲基丙烯酸酯单体组成的内外涂层公开(公告)号：US20060204576A1
公开(公告)日：2006-09-14
申请号：US10532831
申请日：2003-09-04
IPC分类号： A61K9/24
CPC分类号： A61K31/58 , A61K9/1635 , A61K9/209 , A61K9/2846 , A61K9/5026 , A61K9/5078
摘要： The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.
摘要翻译： 本发明涉及一种多层剂型，其包括：a）中性核; b）由甲基丙烯酸酯共聚物组成的内涂层; c）由共聚物组成的外涂层，其中40至95重量％由丙烯酸或甲基丙烯酸的C 4-14烷基酯的自由基聚合的C 1〜 并且其中5至60重量％由在烷基中具有阴离子基团的（甲基）丙烯酸酯单体组成。 本发明的特征在于，内涂层基本上由甲基丙烯酸酯共聚物组成，其中至少高达90重量％由具有中性自由基的（甲基）丙烯酸酯单体组成，其根据DIN 53787具有最小值 成膜温度不高于30℃，含有结合形式的药物活性物质。
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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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