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    • 8. 发明授权
    • Manufacture of oral dosage forms delivering both immediate-release and sustained-release drugs
    • 制备立即释放和持续释放药物的口服剂型
    • US06682759B2
    • 2004-01-27
    • US10066146
    • 2002-02-01
    • Jong C. LimJohn N. Shell
    • Jong C. LimJohn N. Shell
    • A61K922
    • A61K9/209A61K31/155A61K2300/00
    • A method is disclosed for manufacturing a pharmaceutical tablet for oral administration, the tablet combining both immediate-release and prolonged-release modes of drug delivery and using an immediate-release drug that is either insoluble in water or only sparingly soluble and is present in a very small amount compared to the prolonged-release drug. The method involves the use of particles of the immediate-release drug that are equal to or less than 10 microns in diameter, applied as a layer or coating over a core of the prolonged-release drug, the layer or coating being either the drug particles themselves, applied as an aqueous suspension, or a solid mixture containing the drug in admixture with a material that disintegrates rapidly in gastric fluid. The result in both cases is a high degree of uniformity in the proportions of the immediate-release and prolonged-release drugs, uniformity that is otherwise difficult to achieve in view of the insolubility of the immediate-release drug and its relatively small amount compared to the prolonged-released drug.
    • 公开了用于制造用于口服给药的药物片剂的方法,所述药片结合药物递送的立即释放和延长释放模式并且使用不溶于水或仅溶于微溶并且存在于 与延长释放药物相比非常少量。 该方法包括使用直径为等于或小于10微米的速释药物的颗粒,作为延长释放药物的核心上的层或涂层施用,该层或涂层是药物颗粒 或者含有药物的固体混合物与在胃液中快速分解的物质混合。 两种情况的结果是立即释放和延长释放药物的比例高度均匀,鉴于立即释放药物的不溶性而难以实现的均匀性,并且相对于 延长释放的药物。