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    • 1. 发明申请
    • Method For Producing An Oral Pharmaceutical Form With Immediate Disintegration And Active Ingredient Release
    • 生产具有立即崩解和活性成分释放的口服药物形式的方法
    • US20130071475A1
    • 2013-03-21
    • US13677740
    • 2012-11-15
    • Hans-Ulrich PETEREITChristian MEIERAndreas GRYCZKE
    • Hans-Ulrich PETEREITChristian MEIERAndreas GRYCZKE
    • A61J3/10A61K31/192A61K9/14
    • A61J3/10A61K9/0056A61K9/146A61K9/1647A61K9/2054A61K31/192
    • 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.
    • 本发明涉及一种生产口服给药方法,该方法立即分解并释放口腔内的活性成分。 根据所述方法,(a)阴离子药物活性成分与(b)由丙烯酸或甲基丙烯酸的自由基聚合的C1-C4酯和含有官能叔氨基的其它(甲基)丙烯酸酯单体组成的共聚物强烈混合, 和(c)5-50wt。 %的(b)相对于熔融物质中的C 12 -C 22羧酸; 将混合物固化并研磨形成含有平均粒径为200μm以下的活性成分的粉末; 并将粉末包封在由药学上标准的佐剂组成的水溶性基质中,条件是不超过3wt。 相对于共聚物,HLB值至少为14的乳化剂的%必须包含在其中。 本发明还涉及含有活性成分的粉末及其用途。
    • 6. 发明申请
    • COATED PHARMACEUTICAL OR NUTRACEUTICAL PREPARATION WITH ACCELERATED CONTROLLED ACTIVE SUBSTANCE RELEASE
    • 加速控制的活性物质释放的包装药物或营养制剂
    • US20110070302A2
    • 2011-03-24
    • US12742263
    • 2008-02-01
    • Hema RAVISHANKARHans-Ulrich PETEREITShradda BODINGE
    • Hema RAVISHANKARHans-Ulrich PETEREITShradda BODINGE
    • A61K9/32A61K9/00A61K31/522A61P43/00
    • A61K9/5026A61K9/5078
    • The present invention relates to pharmaceutical or nutraceutical preparations comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid, and to tablets and capsules containing same.
    • 本发明涉及药物或营养制剂,其包含a)含有药学或营养物质活性物质的核心; 和b)围绕芯的控制层,其包含i)55至92重量%,基于存在于由80重量份组成的多个(甲基)丙烯酸酯共聚物的一种或多种混合物的层中的(甲基)丙烯酸共聚物的总重量 至(甲基)丙烯酸共聚物的重量比为基于(甲基)丙烯酸的C1至C4烷基酯的结构单元的(甲基)丙烯酸共聚物的重量计为98重量%,以及(甲基)丙烯酸共聚物的重量为2至20重量% 衍生自烷基中具有季铵基团的(甲基)丙烯酸酯单体的结构单元; 和ii)8至45重量%,基于存在于由多于5至59重量%组成的(甲基)丙烯酸酯共聚物的一种或多种的(甲基)丙烯酸酯共聚物的层中的(甲基)丙烯酸共聚物的总重量) 衍生自丙烯酸或甲基丙烯酸的结构单元的共聚物的重量,以及含有它们的片剂和胶囊的重量。