PROCESS FOR PREPARING A GRANULATED PRODUCT FROM A POWDER COMPOSITION
    1.
    发明申请
    PROCESS FOR PREPARING A GRANULATED PRODUCT FROM A POWDER COMPOSITION 审中-公开
    从粉末组合物制备颗粒状产品的方法

    公开(公告)号:US20150290136A1

    公开(公告)日:2015-10-15

    申请号:US14646569

    申请日:2013-02-28

    IPC分类号: A61K9/16

    摘要: The invention discloses a process for preparing granulated product from a powder composition comprising the mixed components (a) and (b) and (c) or (d) or both, with (a), a copolymer consisting of free-radical-polymerized C1- to C4-esters of acrylic or methacrylic acid and alkyl(meth)acrylate monomers with tertiary amino groups in the alkyl side groups (b) 5 to 25% by weight, based on (a), of a C12- to C18-monocarboxylic acid or a C12- to C18-alcohol, (c) 0 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms, (d) 0 to 20% by weight, based on (a), of an emulsifier having an HLB of at least 14, wherein the mixed components are processed by a dry granulation process to a granulate with a mean particle size of 2 mm or less.

    摘要翻译: 本发明公开了一种由包含混合组分(a)和(b)和(c)或(d)或两者的粉末组合物制备造粒产物的方法与(a)由自由基聚合的C1 - 丙烯酸或甲基丙烯酸的C 4-酯和(甲基)丙烯酸烷基酯单体与烷基侧基中的叔氨基(b)基于(a)的5-25重量%的C12- C18-单羧酸 (c)基于(a)基于(a)的碳原子数为3〜10的二羧酸为0〜10重量%,(c)0〜10重量%,(d)0〜20重量% 的具有至少14的HLB的乳化剂,其中所述混合组分通过干法制粒法加工成平均粒径为2mm或更小的颗粒。

    COATING COMPOSITION
    5.
    发明申请
    COATING COMPOSITION 审中-公开
    涂料组合物

    公开(公告)号:US20160193182A1

    公开(公告)日:2016-07-07

    申请号:US14911491

    申请日:2014-08-01

    IPC分类号: A61K31/40 A61K9/50 A61K9/28

    摘要: The invention refers to a coating composition which, calculated on dry weight, is comprising at least 20% by weight polyvinyl alcohol and 0.1 to 20% by weight, calculated on the weight of the polyvinyl alcohol, of a water-insoluble (meth)acrylate copolymer comprising quaternary ammonium groups, wherein the viscosity of an aqueous dispersion comprising that coating composition with 25% (w/w) solid content at 22° C. is 200 mPa·s or less.

    摘要翻译: 本发明涉及一种涂料组合物,其以干重计算,包含至少20重量%的聚乙烯醇和0.1至20重量%,以聚乙烯醇的重量计,水不溶性(甲基)丙烯酸酯 包含季铵基的共聚物,其中包含在22℃下具有25%(w / w)固体含量的涂料组合物的水性分散体的粘度为200mPa·s或更低。

    MULTIPARTICULATE PHARMACEUTICAL COMPOSITION COMPRISING A MULTITUDE OF TWO KINDS OF PELLETS
    6.
    发明申请
    MULTIPARTICULATE PHARMACEUTICAL COMPOSITION COMPRISING A MULTITUDE OF TWO KINDS OF PELLETS 审中-公开
    多种药物组合物,包含两种细胞的多种

    公开(公告)号:US20150366825A1

    公开(公告)日:2015-12-24

    申请号:US14764804

    申请日:2013-04-25

    摘要: Multiparticulate pharmaceutical composition comprising a multitude of two kinds of pellets, A and B, each comprising metoprolol or a pharmaceutically acceptable salt thereof as an active pharmaceutical ingredient, wherein the pellets A are coated with a coating layer comprising at least 30% by weight of a polymeric compound consisting of one or more (meth)acrylate copolymers polymerized from 20 to 40% by weight of ethyl acrylate, 60 to 80% by weight of methyl methacrylate and 0 or less than 5% by weight of methacrylic acid or acrylic acid, in an amount sufficient to result in an active pharmaceutical ingredient release profile according to USP in pH 6.8 test medium with a release rate of less than 20% after 4 hours, wherein the pellets B are not coated or coated with a coating layer and show an active pharmaceutical ingredient release profile according to USP in pH 6.8 test medium with an active pharmaceutical ingredient release rate of more than 40% after 4 hours, wherein the metoprolol release rate of the pellets A in pH 1.2 test medium according to USP with the addition of 40% (v/v) ethanol is •not more than 15% after 15 minutes •more than 15 up to 40% after 30 minutes, wherein the metoprolol release rate of the pellets B in pH 1.2 test medium according to USP with the addition of 40% (v/v) ethanol is •more than 15% after 15 minutes •more than 40% after 30 minutes and wherein the pellets A and B are present in the multiparticulate pharmaceutical composition in a relation resulting in a combined active pharmaceutical ingredient release profile of the multiparticulate pharmaceutical composition according to USP in pH 6.8 test medium with releases rates of •not more than 25% after 1 hour •20 to 40% after 4 hours •40 to 60% after 8 hours •not less than 80% after 20 hours.

    摘要翻译: 包含多种两种丸剂A和B的多片剂药物组合物,A和B各自包含美托洛尔或其药学上可接受的盐作为活性药物成分,其中颗粒A涂覆有包含至少30重量% 由一种或多种(甲基)丙烯酸酯共聚物组成的高分子化合物,其由20至40重量%的丙烯酸乙酯,60至80重量%的甲基丙烯酸甲酯和0或小于5重量%的甲基丙烯酸或丙烯酸聚合, 足以导致根据USP在pH 6.8测试培养基中具有活性药物成分释放曲线的量,其中4小时后释放速率小于20%,其中颗粒B未涂覆或涂覆有涂层并显示活性物质 根据USP在pH 6.8测试培养基中的药物成分释放曲线,4小时后活性药物成分释放速率大于40%,其中美托洛尔 在加入40%(v / v)乙醇的根据USP的pH 1.2测试培养基中的丸粒A的释放速率为15分钟后不超过15%•30分钟后超过15%至40%,其中 在加入40%(v / v)乙醇的根据USP的pH 1.2测试培养基中的丸粒B的美托洛尔释放速率为15分钟后超过15%•30分钟后超过40%,并且其中颗粒A 和B以多颗粒药物组合物的形式存在,其导致根据USP在pH 6.8测试培养基中的多颗粒药物组合物的组合的活性药物成分释放曲线,1小时后释放速率为不超过25%•20至 4小时后40%•8小时后40-60%•20小时后不少于80%。

    PROCESS FOR PREPARING AQUEOUS DISPERSIONS
    8.
    发明申请
    PROCESS FOR PREPARING AQUEOUS DISPERSIONS 审中-公开
    制备水性分散体的方法

    公开(公告)号:US20150250888A1

    公开(公告)日:2015-09-10

    申请号:US14430592

    申请日:2012-11-27

    IPC分类号: A61K47/32 A61K9/10

    CPC分类号: A61K47/32 A61K9/10 A61K9/2846

    摘要: The invention discloses a process for preparing aqueous dispersions comprising the components (a) and (b) and optionally (c) or (d) or both, (a) a copolymer consisting of free-radical-polymerized C1- to C4-esters of acrylic or methacrylic acid and alkyl(meth)acrylate monomers with tertiary ammonium groups in the alkyl side groups, (b) 5 to 25% by weight, based on (a), of a C12- to C18-monocarboxylic acid or a C12- to C18-alcohol, (c) 0 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms, (d) 0 to 20% by weight, based on (a), of an emulsifier having an HLB of at least 14 by dispersing the components in water where the water has a temperature of more than 40 and up to 85° C., where the solid content of the dispersion is from 5 to 40% by weight and where a clear colloidal dispersion is obtained in less than 30 min.

    摘要翻译: 本发明公开了一种制备包含组分(a)和(b)和任选地(c)或(d)或两者的水分散体的方法,(a)由游离基聚合的C 1 -C 4酯 丙烯酸或甲基丙烯酸和烷基侧基具有叔铵基的(甲基)丙烯酸烷基酯单体,(b)基于(a)的5-25重量%的C12- C18-一元羧酸或C12- (c)0至10重量%,基于(a)具有3至10个碳原子的二羧酸,(d)0至20重量%(a),基于(a)的乳化剂,其具有 通过将组分分散在水中,其中水的温度高于40℃且高达85℃,其中固体含量为5至40重量%,并且其中透明胶体 在少于30分钟内获得分散体。