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    • 2. 发明申请
    • SOLID PHARMACEUTICAL DOSAGE FORMS
    • 固体药物剂型
    • WO2015140709A1
    • 2015-09-24
    • PCT/IB2015/051944
    • 2015-03-17
    • NOVARTIS AGDEODHAR, UnmeshZHANG, LeiBABU, Sreehari
    • DEODHAR, UnmeshZHANG, LeiBABU, Sreehari
    • A61K9/20A61K31/135A61K31/352
    • A61K31/357A61K9/2077A61K31/137A61K31/366A61K45/06Y02A50/411A61K2300/00
    • The present invention relates to the use of active pharmaceutical ingredients (API) as lubricant and/or antiadherent in the manufacturing of solid pharmaceutical dosage forms. It further relates to solid pharmaceutical dosage forms the production of which involves a granulation process step followed by a capsule filling or tablet compression step. Said pharmaceutical dosage form is comprised of an intragranular phase and an extragranular phase wherein the latter is comprised of one or more active pharmaceutical ingredients (API) which functions as lubricants and/or antiadherents in the manufacturing of said solid dosage form. Specifically, the API Artemether with its endoperoxide structural element was surprisingly found to exhibit lubricant and/or antiadherent effects when used extragranularly. In further aspects, the present invention relates to the manufacturing process to produce said pharmaceutical dosage forms as well as to a test method to determine whether an API functions as lubricant and/or antiadherent.
    • 本发明涉及在制备固体药物剂型中使用活性药物成分(API)作为润滑剂和/或抗粘附剂。 它还涉及固体药物剂型,其生产包括造粒工艺步骤,随后是胶囊填充或片剂压片步骤。 所述药物剂型由晶内相和颗粒外晶相组成,其中后者由制备所述固体剂型的一种或多种活性药物成分(API)组成,其作为润滑剂和/或抗粘附剂起作用。 具体地说,具有其内过氧化物结构元件的API蒿甲醚被惊奇地发现在粒子外使用时表现出润滑剂和/或抗附着效应。 在其它方面,本发明涉及生产所述药物剂型的制备方法以及用于确定API是否用作润滑剂和/或抗粘附剂的测试方法。