Opioid agonist/antagonist combinations in controlled release dosage form

摘要

An oral dosage form, comprising an orally therapeutically effective amount of an opioid agonist, and an opioid antagonist and a sustained release carrier, the dosage form having a ratio of opioid antagonist to opioid agonist that provides a combination product which is analgesically effective when the combination is administered orally, but which (i) is aversive in physically dependent human subjects when administered at the same dose or at a higher dose than the the therapeutically affective dose and (ii) maintains an analgesic effect but does not increase analgesic efficacy of the opioid agonist relative to the same therapeutic dose of opioid analgesic when administered to human patients without sthe opioid antagonist; the dosage form providing a release of the opioid agonist and antagonist indicative of twice-a-day therapy. Figure 1 shows naltrexone antagonism of hydrocodone-induced VAS (Visual Analogue Scale) "drug effect" for Example 1.