Opioid agonist/opioid antagonist/acetaminophen combinations
AssigneeEuro-Celtique S.A.
InventorsRobert F. Kaiko, Robert D. Colucci
Life of this patent
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Abstract
The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen 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).
Claims55
An oral dosage form, comprising
- an orally therapeutically effective amount of
- (A) an opioid agonist;
- (B) acetaminophen;
- and
- (C) an opioid antagonist;
- the dosage form having a ratio of opioid antagonist to opioid agonist to acetaminophen 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 in the same amount or in a higher amount than said therapeutically effective amount;
- and (ii) maintains an analgesic effect but does not increase analgesic efficacy of the opioid agonist together with the acetaminophen relative to the same therapeutic amount of opioid analgesic together with the acetaminophen when administered to human patients without said opioid antagonist.
A method of treating pain, comprising:
- administering an oral dosage form which contains a therapeutically effective amount of
- (A) an opioid agonist;
- (B) acetaminophen;
- and
- (C) an opioid antagonist;
- the dosage form having a ratio of opioid antagonist to opioid agonist to acetaminophen that provides a combination product which is analgesically effective when the combination is administered orally, but (i) is aversive in physically dependent human subjects when administered in the same amount or a higher amount than said therapeutically effective amount;
- and (ii) maintains an analgesic effect but does not increase analgesic efficacy of the opioid analgesic together with the acetaminophen relative to the same therapeutic amount of opioid analgesic together with the acetaminophen when administered to human patients without said opioid antagonist.
A method of preventing oral abuse of an oral opioid formulation, comprising:
- preparing an oral dosage form which comprises a therapeutically effective amount of
- (A) an opioid agonist;
- (B) acetaminophen;
- and
- (C) an opioid antagonist;
- the dosage form having a ratio of opioid antagonist to opioid agonist to acetaminophen that provides a combination product which is analgesically effective when the combination is administered orally, but (i) is aversive in physically dependent human subjects when administered in the same amount or a higher amount than said therapeutically effective amount;
- and (ii) maintains an analgesic effect but does not increase analgesic efficacy of the opioid analgesic together with the acetaminophen relative to the same therapeutic amount of opioid analgesic together with the acetaminophen when administered to human patients without said opioid antagonist.
An oral dosage form, comprising:
- an orally therapeutically effective amount of
- (A) an opioid agonist;
- (B) acetaminophen;
- and
- (C) an opioid antagonist;
- the dosage form having a ratio of opioid antagonist to opioid agonist to acetaminophen 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 in the same amount or a higher amount than said therapeutically effective amount;
- and (ii) maintains or decreases analgesic efficacy of the opioid agonist together with the acetaminophen relative to the same therapeutic amount of opioid analgesic together with the acetaminophen when administered to human patients without said opioid antagonist.
Dependencies are inferred from the claim text.