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    Homogeneous preformulations containing high concentrations of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations
    1.
    发明授权
    Homogeneous preformulations containing high concentrations of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations 失效
    含有高浓度类固醇的均质预制品，用于生产低剂量固体和半固体药物制剂

    公开(公告)号：US06290931B1

    公开(公告)日：2001-09-18

    申请号：US09319802

    申请日：1999-06-10

    申请人： Detlef Grawe ,  Peter Hoesel ,  Peter Moellmann ,  Carsten Timpe ,  Michael Dittgen ,  Klaus Matthey

    发明人： Detlef Grawe ,  Peter Hoesel ,  Peter Moellmann ,  Carsten Timpe ,  Michael Dittgen ,  Klaus Matthey

    IPC分类号： A61K912

    CPC分类号： A61K31/569 ,  A61K9/1623 ,  A61K9/1676 ,  A61K31/567 ,  A61K31/575

    摘要： A homogeneous steroid-containing preformulation for production of solid and semi-solid pharmaceutical preparations containing a uniform constant dosage of at least one steroid in a range from 0.001 to 1 percent by weight is described. This steroid-containing preformulation contains of from 0.001 to 50 percent by weight of the at least one steroid. The homogeneous steroid-containing preformulation is made by a method including dissolving the at least one steroid in a solvent to form a dispersant; dispersing an adjuvant consisting of adjuvant particles in the dispersant in a mass ratio of the adjuvant to the at least one steroid of 1:1 to 1000:1 to form a suspension; and creating a spray-mist of the suspension so as to evaporate and remove the solvent from the suspension and thus to form a dried particulate which includes steroid-containing particles. The droplets in the spray mist have a droplet diameter greater than a mean diameter of the adjuvant particles. The maximum particle size of the dried particulate forming the steroid-containing preformulation is increased by less than 30 percent in comparison to an average particle size of the adjuvant particles.

    摘要翻译： 描述了用于生产固体和半固体药物制剂的均匀类固醇预制剂，其含有0.001至1重量％范围内的至少一种类固醇的均匀恒定剂量。 该含类固醇的预制剂含有0.001至50重量％的至少一种类固醇。 通过包括将至少一种类固醇溶解在溶剂中以形成分散剂的方法制备含均匀类固醇的预配制剂; 将助剂颗粒组成的佐剂以佐剂与至少一种类固醇的质量比为1:1至1000:1分散在分散剂中以形成悬浮液; 并产生悬浮液的喷雾，从而从悬浮液中蒸发除去溶剂，从而形成包含类固醇颗粒的干燥颗粒。 喷雾中的液滴的液滴直径大于辅助颗粒的平均直径。 与佐剂颗粒的平均粒径相比，形成含类固醇的预制剂的干燥颗粒的最大粒度增加小于30％。

    Laminates containing an active substance transdermal system
    2.
    发明授权
    Laminates containing an active substance transdermal system 有权
    含有活性物质透皮系统的层压体

    公开(公告)号：US06902741B1

    公开(公告)日：2005-06-07

    申请号：US09913112

    申请日：2000-02-08

    申请人： Detlef Grawe ,  Peter Hoesel ,  Wilfried Fischer

    发明人： Detlef Grawe ,  Peter Hoesel ,  Wilfried Fischer

    IPC分类号： A61K9/14 ,  A61K9/70 ,  A61K31/568 ,  A61P5/24 ,  A61F13/02 ,  A61L15/16

    CPC分类号： A61K9/7053 ,  A61K9/146

    摘要： The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.

    摘要翻译： 透皮系统包括含有性激素的粘合剂基质，其在溶解或分散形式的亲水性非交联聚合物中含有性激素的夹杂物。 夹杂物的浓度为性激素的20〜90重量％，超过50重量％的非晶体。 亲水性非交联聚合物可以是聚乙烯吡咯烷酮，甲基纤维素，乙基纤维素或羟乙基纤维素。 粘合剂基质可以是聚异丁烯，乙烯 - 乙酸乙烯酯共聚物或聚苯乙烯 - 丁二烯嵌段共聚物。