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COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG
COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG
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机译:发挥滥用潜能并延长药物作用时间的化合物和方法
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摘要
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.
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