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    • 3. 发明申请
    • COMPOSITIONS IN POWDER FORM MADE OF SOFT AGGLOMERATES OF A MICRONIZED DRUG AND OF A TWO-COMPONENTS EXCIPIENT, AND PROCESS FOR THEIR PREPARATION
    • 一种微量药物和两种组分的软组合粉末形式的组合物及其制备方法
    • US20100233276A1
    • 2010-09-16
    • US12734300
    • 2007-10-26
    • Renata RaffinPaolo ColomboFabio SonvicoGaia ColomboAlessandra RossiFrancesca Buttini
    • Renata RaffinPaolo ColomboFabio SonvicoGaia ColomboAlessandra RossiFrancesca Buttini
    • A61K9/14A61K9/50A61K9/58A61K9/60A61K9/62A61K9/64
    • A61K9/1617A61K9/1623
    • The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20%, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface. By tumbling, the surface-active agent present on microparticles excipient surface was spread to fill the inter-particle interstices of drug particles giving rise to more resistant agglomerates. This phenomenon occurred also by vibration; the production in this case was quicker.
    • 与赋形剂微粒混合的药物微粒的所述团聚是用于通过造粒或压实技术损坏的微粉化产品的尺寸增大的技术。 这些附聚物可以作为口服或缓释剂型使用,或者分散在液体中。 赋形剂微粒的组成和数量是聚集质量的关键因素。 因此,调整表面活性剂的含量在8〜20%之间,赋形剂微粒可能聚集本身不能团聚的药物微粒。 增加喷雾干燥的赋形剂微粒中的表面活性剂浓度或增加共混物中这些赋形剂微粒的分数,聚集得到改善。 喷雾干燥技术将表面活性剂浓缩在微粒表面上。 通过翻滚,存在于微粒赋形剂表面上的表面活性剂被扩散以填充药物颗粒的颗粒间隙,从而产生更多的抗凝结物质。 这种现象也是由振动引起的。 在这种情况下的生产更快。