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    • 7. 发明授权
    • Process for the preparation of shaped, compressed controlled-release
unit-dosage forms, and the compressed unit-dosage forms thus obtained
    • 用于制备成形压缩的控释单元剂型的方法以及由此获得的压缩的单位剂型
    • US5840330A
    • 1998-11-24
    • US357143
    • 1994-12-15
    • Berthold StemmleKlaus BuddeAlexander WirlFritz Demmer
    • Berthold StemmleKlaus BuddeAlexander WirlFritz Demmer
    • A61K9/22A61K20060101A61K9/20A61K31/19A61K47/00A61P3/06
    • A61K9/2095A61K9/2077
    • Process for the preparation of shaped, compressed controlled-release unit-dosage forms from a therapeutic active substance exhibiting a self-retarding release that depends on the magnitude of the force used for the compression. The process gives unit-dosage forms for which the release of the active substance is highly uniform, reproducibly identical and largely linear. To achieve this, the active substance and an additive charge that inhibits or compensates for the self-retardation of its release are processed into particles in the first stage of production, so that the preliminary compressed objects made from these particles without any further additives exhibit a rapid release (in comparison with the required controlled release) over the range of the force of compression envisaged for the production of the unit-dosage form in question, after which the particles are compressed in the second stage of production with a release-retarding agent to obtain the unit-dosage forms. The invention also relates to the unit-dosage forms thus obtained.
    • 从治疗活性物质制备成形的,压缩的控制释放单位剂型的方法,其表现出取决于用于压缩的力的大小的自我缓解释放。 该方法给出了单位剂型,其中活性物质的释放是高度均匀的,可重复地相同的并且在很大程度上是线性的。 为了达到这个目的,在生产的第一阶段,抑制或补偿其释放的自我延迟的活性物质和添加剂被加工成颗粒,使得由这些颗粒制成的预先压制的物体没有任何其它添加剂显示出 在生产所述单位剂量形式的压缩力的范围内快速释放(与所需的控制释放相比),然后在第二阶段用释放阻滞剂压缩颗粒 以获得单位剂型。 本发明还涉及由此获得的单位剂型。