Direct Compression Formulation and Process
    10.
    发明申请
    Direct Compression Formulation and Process 审中-公开
    直接压缩配方和工艺

    公开(公告)号:US20140205663A1

    公开(公告)日:2014-07-24

    申请号:US14226871

    申请日:2014-03-27

    IPC分类号: A61K9/20 A61K31/40 C07D207/16

    摘要: Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of direct compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus present formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.

    摘要翻译: 可以是98.5-100%纯度的二肽基肽酶IV抑制剂(本文中称为DPP-IV)是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物,例如具有所需硬度,崩解性的片剂和胶囊 能力和可接受的溶出特性。 DPP-IV不是固有的可压缩性,因此存在配方问题。 制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。 最佳流量有助于均匀的模头填充和重量控制。 使用的粘合剂确保足够的内聚性质,使DPP-IV能够使用直接压缩方法进行压缩。 所制备的片剂提供可接受的体外溶出曲线。