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    • 10. 发明申请
    • METHYLPHENIDATE MODIFIED RELEASE FORMULATIONS
    • 甲基苯酚改性释放配方
    • WO02034234A2
    • 2002-05-02
    • PCT/US2001/042561
    • 2001-10-09
    • A61K9/22A61K9/50A61K9/54A61K9/56A61K9/58A61K9/62A61K31/4458A61K47/14A61K47/26A61K47/30A61K47/32A61K47/36A61K47/38A61K9/00
    • A61K31/4458A61K9/5078A61K9/5084
    • A pharmaceutical MR (modified release) multiparticulate dosage form such as a capsule (once-a-day MR Capsule) of Methylphenidate indicated for the treatment of children with attention deficit hyperactivity disorder (ADHD), capable of delivering a portion of the dose for rapid onset of action and the remainder of the dose in a controlled manner for about 12 hours, is composed of a multitude of multicoated particles made of two populations of drug layered beads, IR (immediate release) and ER (extended release) Beads. The IR beads preferably are made by layering an aqueous solution comprising a drug and a binder on to non-pareil sugar spheres and then applying a seal coat to the drug coated cores. The ER Beads are made by applying an extended release coating of a water insoluble dissolution rate controlling polymer such as ethylcellulose to IR Beads. The MR Capsules are manufactured by filling IR and ER Beads in a proper ratio; the dose and the ratio required for an efficacious, cost effective and patient compliant treatment of children with ADHD were determined from extensive clinical investigations and in vitro/in vivo correlations performed as per FDA Guidelines, Guidance for Industry: Extended Release Oral Dosage Forms.
    • 药物MR(改性释放)多颗粒剂型,例如哌甲酯的胶囊(每日一次MR胶囊),用于治疗注意缺陷多动障碍(ADHD)的儿童,能够递送一部分剂量用于快速 起始作用和其他剂量以受控方式进行约12小时,由多个由多种药物分层珠,IR(即时释放)和ER(延长释放)珠组成的多层颗粒组成。 IR珠优选通过将包含药物和粘合剂的水溶液层压到非帕里儿糖球上,然后将涂层涂覆到药物包衣的核心上来制备。 ER珠是通过将不溶于水的溶解速率控制聚合物如乙基纤维素的延长释放涂层施加到IR珠而制成的。 MR胶囊通过以适当的比例填充IR和ER珠来制造; 根据FDA指南“行业指南”进行的广泛临床研究和体外/体内相关性测定了对ADHD儿童进行有效,成本效益和患者适应性治疗所需的剂量和比例。 延长口服剂型。