Opioid agonist/antagonist combinations
AssigneeEuro-Celtique S.A.
InventorsRobert F. Kaiko, Robert D. Colucci
Life of this patent
Estimating the term…
Abstract
The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).
Claims63
A sustained release oral dosage form, comprising an orally therapeutically effective dose of an opioid agonist, an opioid antagonist, and a sustained release carrier, said 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 said therapeutically effective 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 said opioid antagonist;
- such that the dosage form is administrable on a twice-a-day or on a once-a-day basis.
A method of treating oral abuse of an oral opioid formulation, comprising preparing a sustained release oral dosage form which comprises a therapeutically effective dose of an opioid agonist and a sustained release carrier and incorporating therein an opioid antagonist in a ratio to said opioid agonist such that the oral dosage form is analgesically effective when administered orally, but (i) is aversive in physically dependent human subjects when administered at the same dose or at a higher dose than said therapeutically effective 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 said opioid antagonist.
A sustained release oral dosage form, comprising an orally therapeutically effective dose of an opioid agonist, an opioid antagonist, and a sustained release carrier, said 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 said therapeutically effective dose;
- and (ii) maintains or decreases analgesic efficacy of the opioid agonist relative to the same therapeutic dose of opioid analgesic when administered to human patients without said opioid antagonist;
- such that the dosage form is administrable on a once-a-day basis.
Dependencies are inferred from the claim text.