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    • 1. 发明授权
    • Effervescent granules and methods for their preparation
    • 泡腾颗粒及其制备方法
    • US06488961B1
    • 2002-12-03
    • US09468513
    • 1999-12-21
    • Joseph R RobinsonJames W. McGinity
    • Joseph R RobinsonJames W. McGinity
    • A61K946
    • A61K9/0007A61K9/1694
    • Disclosed here are effervescent granules having a controllable rate of effervescence. In some embodiments, the such granules comprise an acidic agent, an alkaline agent, a pharmacologically active agent, hot-melt extrudable binder capable of forming a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process. The present invention also provides a thermal heat process for preparing a pharmacologically active agent containing effervescent granule. In certain aspects, the granules contain pharmacologically active agents such as narcotics, antidiarrheal agents, antiviral agents, anxiolytic agents, a cholesterol lowering agent, an alpha adrenergic blocking agent, a phenanthrene derivative. By way of example, some of the narcotics that may be included in the granules and in the process of preparing the granules include, by way of example: phenanthrene derivatives (e.g., morphine sulfate), and morphine derivatives (e.g., hydromorphone hydrochloride).
    • 这里公开了具有可控的泡腾速率的泡腾颗粒。 在一些实施方案中,这种颗粒包含酸性试剂,碱性试剂,药理学活性剂,能够与酸性试剂形成共晶混合物的热熔可挤出粘合剂和任选的增塑剂。 泡腾颗粒通过热熔挤出方法制成。 本发明还提供了制备含有泡腾颗粒的药理活性剂的热加工方法。 在某些方面,颗粒含有药理学活性剂如麻醉剂,止泻药,抗病毒剂,抗焦虑剂,降胆固醇剂,α肾上腺素能阻断剂,菲衍生物。 作为实例,可以包括在颗粒中和在制备颗粒的过程中的一些麻醉剂包括例如:菲衍生物(例如硫酸吗啡)和吗啡衍生物(例如盐酸氢吗啡酮)。