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    • 3. 发明授权
    • Compounds and methods for lowering the abuse potential and extending the duration of action of a drug
    • 用于降低滥用潜力并延长药物作用时间的化合物和方法
    • US07230005B2
    • 2007-06-12
    • US10800898
    • 2004-03-15
    • Jules A. ShaferVladislav V. TelyatnikovZhiwei Guo
    • Jules A. ShaferVladislav V. TelyatnikovZhiwei Guo
    • A61K31/485C07D489/02
    • C07D489/08A61K47/555A61K47/60
    • The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.
    • 降低生物可利用药物如鸦片止痛剂的滥用潜力,并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。 与活性药物的许多现有持续释放制剂不同,其中通过咀嚼,破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂,这种包含本发明前药的片剂或胶囊珠粒的机械加工 既不释放活性药物也不妥协药物对药物的受控转化。 此外,含有本发明前药或其他药物的片剂和胶囊珠可以用足量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制,以阻止对这些给药模式未注明的制剂的不适当的静脉内和鼻内施用。