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    • 85. 发明申请
    • Method for producing an immediately decomposing oral form of administration which releases active ingredients
    • 用于产生释放活性成分的立即分解口服给药形式的方法
    • US20060051412A1
    • 2006-03-09
    • US10542283
    • 2003-11-21
    • Hans-Ulrich PetereitChristian MeierAdreas Gryczke
    • Hans-Ulrich PetereitChristian MeierAdreas Gryczke
    • A61K9/20B27N3/00
    • 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)由丙烯酸的自由基聚合的C 1 -C 4 -C 4酯的共聚物密集混合 或甲基丙烯酸和其它含有官能叔氨基的(甲基)丙烯酸酯单体,和(c)5-50wt。 %)相对于(b)相对于熔融物质中的C 12 -C 22 -C 22羧酸; 将混合物固化并研磨形成含有平均粒径为200μm或更小的活性成分的粉末; 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。
    • 87. 发明授权
    • Coated medicament forms with controlled active substance release
    • 具有受控活性物质释放的涂层药物形式
    • US06878387B1
    • 2005-04-12
    • US09787438
    • 1999-09-28
    • Hans-Ulrich PetereitThomas BeckertEva Lynenskjold
    • Hans-Ulrich PetereitThomas BeckertEva Lynenskjold
    • A61K47/32A61K9/22A61K9/32A61K9/50A61K9/52A61K9/58A61K9/64A61K31/522A61K47/12A61P11/06C08F220/18C08L33/04A61K9/14A61K9/16A61K9/46A61K9/48
    • A61K9/5078A61K9/5026A61K31/522
    • 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.
    • 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。