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    • 1. 发明申请
    • IMMEDIATE RELEASE DRUG FORMULATION COMBINING OPIOID AND NONOPIOID ANALGESICS WITH ABUSE DETERRENCE AND OVERDOSE PROTECTION
    • 立即释放药物制剂与阿片类药物和非甾体类镇痛药物的不良反应和过量保护
    • WO2017192608A1
    • 2017-11-09
    • PCT/US2017/030667
    • 2017-05-02
    • KASHIV PHARMA LLC
    • VAKA, Siva, Ram KiranMEGHPARA, KanjiDESAI, DipenPHUAPRADIT, WantaneeSHAH, Navnit, H.THONGSUKMAK, Atsawin
    • A61K9/16A61K9/20A61K9/48A61K9/50A61K31/167A61K31/485
    • A61K9/5073A61K9/1611A61K9/1623A61K9/1635A61K9/1641A61K9/1652A61K9/2081A61K9/2086A61K9/48A61K9/5026A61K9/5042A61K9/5047A61K9/5084A61K31/167A61K31/485
    • The present disclosure provides solid immediate release (IR) dosage forms, including particulate and multi-particulate dosage forms, with abuse deterrent and overdose protection characteristics. In certain embodiments, the dosage form is multi¬ particulate, comprising: a first population of particulates comprising a therapeutically effective amount of at least one opioid embedded in a polymer matrix, an optional seal coat, a functional coat layer(s), and an over coat, wherein the functional coat layer(s) comprises a nonionic water-insoluble polymer, and a cationic polymer that dissolves at a pH of less than about 5; a second population of particulates comprising a therapeutically effective amount of acetaminophen (APAP) embedded in a polymer matrix, an optional seal coat, a functional coat layer(s), and an over coat, wherein the functional coat layer(s) comprises a cationic polymer that dissolves at a pH of less than about 5 and an optional nonionic water-insoluble polymer; and a third population of particulates comprising an alkaline agent, and an optional pH-stabilizing agent, wherein the alkaline agent raises the gastric pH when three or more dosage units are ingested, and the pH-stabilizing agent maintains the elevated pH. The dosage forms, including particulate and multi-particulate dosage forms, are designed to accomplish the desired combination of analgesia, abuse deterrence, and overdose protection.
    • 本公开提供了具有滥用威慑和过量保护特征的固体立即释放(IR)剂型,包括颗粒剂和多颗粒剂型。 在某些实施方案中,剂型是多&不; 其包含:第一群粒子,其包含治疗有效量的嵌入聚合物基质中的至少一种阿片样物质,任选的密封包衣,功能包衣层和外包衣,其中功能包衣层 )包含非离子型水不溶性聚合物和在小于约5的pH下溶解的阳离子型聚合物; 包含嵌入聚合物基质中的治疗有效量的对乙酰氨基酚(APAP),任选的密封包衣,功能包衣层和外包衣的第二群颗粒,其中所述功能包衣层包含阳离子 在小于约5的pH下溶解的聚合物和任选的非离子型水不溶性聚合物; 以及第三群颗粒,其包含碱性试剂和任选的pH稳定剂,其中当摄入三个或更多个剂量单位时,所述碱性试剂提高胃的pH,并且所述pH稳定剂保持提高的pH。 包括颗粒剂和多颗粒剂型在内的剂型设计用于实现镇痛,滥用威慑和过量保护的所需组合。