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    • 87. 发明授权
    • Delayed release microtablet of .beta.-phenylpropiophenone derivatives
    • β-苯基苯丙酮衍生物的延迟释放微量片
    • US5681588A
    • 1997-10-28
    • US525749
    • 1995-10-03
    • Karl KolterHelmut FrickeVolker BuehlerHerbert Mueller-Peltzer
    • Karl KolterHelmut FrickeVolker BuehlerHerbert Mueller-Peltzer
    • A61K9/16A61K9/20A61K9/22A61K9/48A61K9/52A61K31/135A61K31/138
    • A61K9/2072A61K31/135A61K31/138A61K9/4808
    • A cylindrical delayed release tablet with a convex or flat upper side and lower side is provided, along with a method for its production and a gelatin capsule containing 3-200 tablets of the same having identical or different release rates, wherein the tablet if made of .beta.-phenylpropiophenone derivatives of the formula I as active ingredient ##STR1## where R is n-propyl or 1,1-dimethylpropyl, and their pharmacologically acceptable salts, wherein the tablet has a height and diameter that are both, independently of one another, 1-3 mm, the active ingredient content is in the range from 81-99.9% of the weight of the microtablet, (but not taking into account the weight of any coating which is present, the active ingredient density is greater than 1, the release of active ingredient in the USP paddle method at 50 rpm is 80% as a maximum after 3 hours and as a minimum after 24 hours, the release rate is virtually independent of the pressure when compressing the tablets, and the tablet contains no release-delaying ancillary substance but can contain 0.1-5% by weight of a lubricant and 0-18.9% by weight of other conventional ancillary substances.
    • PCT No.PCT / EP94 / 00949 Sec。 371 1995年10月3日第 102(e)日期1995年10月3日PCT 1994年3月24日PCT公布。 出版物WO94 / 22434 日期:1994年10月3日提供了具有凸形或平坦的上侧和下侧的圆柱形延迟释放片剂及其制备方法和含有相同或不同释放速率的3-200片的明胶胶囊,其中 片剂如果由式I的β-苯基苯丙酮衍生物作为活性成分,其中R是正丙基或1,1-二甲基丙基,以及它们的药理学上可接受的盐,其中片剂的高度和直径都是 ,彼此独立地为1-3mm,活性成分含量在微片的重量的81-99.9%的范围内(但不考虑存在的任何涂层的重量,活性成分密度 大于1,USP桨法以50rpm的活性成分在3小时后最大释放80%,24小时后最小释放,释放速度基本上与压片时的压力无关, 并且片剂不含释放延迟辅助物质,但可含有0.1-5重量%的润滑剂和0-18.9重量%的其它常规辅助物质。
    • 90. 发明授权
    • Production of pulverulent coating compositions for stable protective coatings for pharmaceutical dosage forms
    • 生产用于药物剂型的稳定保护性涂料的粉末涂料组合物
    • US08865250B2
    • 2014-10-21
    • US13406626
    • 2012-02-28
    • Karl KolterMaximilian AngelBernhard Linner
    • Karl KolterMaximilian AngelBernhard Linner
    • A61K9/28A61K47/32C09D5/03
    • A61K47/32A61K9/2846C09D5/03
    • Described are processes for producing pulverulent coating compositions comprising providing an aqueous polymer dispersion comprising i) as component A a polymer obtained by radical polymerization of a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound selected from esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids with C1-C8-alkanols; and spray processing the aqueous polymer dispersion in the presence of a drying gas to provide a powder, wherein the entry temperature of the drying gas into the spraying apparatus is at least 20° C. above the glass transition temperature and is at least 20° C. above the minimum film-forming temperature of the polymer and the exit temperature of the drying gas from the spraying apparatus is kept at 40 to 85° C.
    • 描述了制备粉状涂料组合物的方法,其包括提供含水聚合物分散体,其包含i)作为组分A的是通过a)N,N-二乙基氨基乙基甲基丙烯酸酯的自由基聚合获得的聚合物,和b)至少一种可自由基聚合的化合物,其选自α ,烯键式不饱和单羧酸和二羧酸与C 1 -C 8 - 链烷醇; 并在干燥气体存在下对聚合物水分散体进行喷雾处理以提供粉末,其中干燥气体进入喷涂装置的入口温度高于玻璃化转变温度至少20℃,并且至少为20℃ 高于聚合物的最低成膜温度和来自喷涂装置的干燥气体的出口温度保持在40至85℃。