Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant agent
Disclosed in certain embodiments is an oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of the dosage form after tampering.
1. A method of preparing a pharmaceutical dosage form comprising combining a therapeutically effective amount of an opioid analgesic, an opioid antagonist and an irritant in a pharmaceutical dosage form, wherein the irritant is in an effective amount to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
2. The method of claim 1 , wherein said irritant is at least partially interdispersed with the opioid analgesic.
3. A method of treating abuse of an oral dosage form of an opioid analgesic comprising: preparing the dosage form with an analgesically effective amount of an opioid analgesic, an opioid antagonist; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
4. The method of claim 3 , wherein the irritant comprises from about 0.00125% to about 50% by weight of the dosage form.
5. The method of claim 4 , wherein the irritant comprises from about 1 to about 7.5% by weight of the dosage form.
6. The method of claim 5 , wherein the irritant comprises from about 1 to about 5% by weight of the dosage form.
7. The method of claim 3 , wherein the opioid antagonist is in an amount to attenuate a side effect of said opioid analgesic selected from the group consisting of anti-analgesia, hyperalgesia, hyperexcitability, physical dependence, tolerance, and a combination of any of the foregoing.
8. The method of claim 3 , wherein the opioid antagonist comprises naloxone or a pharmaceutically acceptable salt thereof.
9. The method of claim 3 , wherein the opioid antagonist comprises naltrexone or a pharmaceutically acceptable salt thereof.
10. The method of claim 3 , wherein the weight ratio of the opioid agonist and the opioid antagonist is from about 1:1 to about 50:1.
11. The method of claim 3 , wherein the opioid analgesic is selected from the group consisting of hydrocodone, morphine, hydromorphone, oxycodone, codeine, levorphanol, meperidine, methadone, oxymorphone, buprenorphine, fentanyl and derivatives thereof, dipipanone, heroin, tramadol, etorphine, dihydroetorphine, butorphanol, levorphanol, salts thereof, and mixtures thereof.
12. The method of claim 11 , wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.
13. The method of claim 1 , wherein the opioid analgesic is selected from the group consisting of hydrocodone, morphine, hydromorphone, oxycodone, codeine, levorphanol, meperidine, methadone, oxymorphone, buprenorphine, fentanyl and derivatives thereof, dipipanone, heroin, tramadol, etorphine, dihydroetorphine, butorphanol, levorphanol, salts thereof, and mixtures thereof.
14. The method of claim 13 , wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.
15. The method of claim 1 , wherein the opioid antagonist comprises naloxone or a pharmaceutically acceptable salt thereof.
16. The method of claim 1 , wherein the opioid antagonist comprises naltrexone or a pharmaceutically acceptable salt thereof.
17. The method of claim 1 , wherein the opioid antagonist is in an amount to attenuate a side effect of said opioid analgesic selected from the group consisting of anti-analgesia, hyperalgesia, hyperexcitability, physical dependence, tolerance, and a combination of any of the foregoing.
18. The method of claim 1 , wherein the irritant comprises from about 0.00125% to about 50% by weight of the dosage form.
19. The method of claim 18 , wherein the irritant comprises from about 1 to about 7.5% by weight of the dosage form.
20. The method of claim 19 , wherein the irritant comprises from about 1 to about 5% by weight of the dosage form.