Method of preventing abuse of opioid dosage forms

Abstract

The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.

1 - 11 . (canceled)  
     
     
         12 . An oral dosage form comprising: 
 (i) an analgesically effective amount of an orally active opioid agonist; and    (ii) naltrexone or a pharmaceutically acceptable salt thereof;    said opioid agonist and naltrexone or pharmaceutically acceptable salt thereof being chosen such that the opioid agonist and the naltrexone or pharmaceutically acceptable salt thereof are only extractable from the dosage form together, and at least a two-step extraction process is required to separate the opioid antagonist from the naltrexone or pharmaceutically acceptable salt thereof, the amount of naltrexone or pharmaceutically acceptable salt thereof included being sufficient to counteract opioid effects if extracted from the oral dosage form together with the opioid agonist and administered parenterally.    
     
     
         13 . The oral dosage form of  claim 12 , wherein the opioid agonist is hydromorphone hydrochloride and the naltrexone or pharmaceutically acceptable salt thereof is naltrexone hydrochloride.  
     
     
         14 . The oral dosage form of  claim 12 , wherein the opioid agonist is oxycodone hydrochloride and the naltrexone or pharmaceutically acceptable salt thereof is naltrexone hydrochloride.  
     
     
         15 . The oral dosage form of  claim 12 , wherein the opioid agonist is morphine sulfate and the naltrexone or pharmaceutically acceptable salt thereof is naltrexone hydrochloride.  
     
     
         16 . The oral dosage form of  claim 12 , wherein the opioid agonist is hydrocodone bitartrate and the naltrexone or pharmaceutically acceptable salt thereof is naltrexone hydrochloride.  
     
     
         17 . The oral dosage form of  claim 12 , wherein the opioid agonist is hydromorphone hydrochloride and the ratio of said naltrexone to said hydromorphone is from about 0.148:1 to about 1.185:1 by weight.  
     
     
         18 . The oral dosage form of  claim 12 , wherein the opioid agonist is hydromorphone hydrochloride and the ratio of said naltrexone to said hydromorphone is from about 0.222:1 to about 0.111:1 by weight.  
     
     
         19 . The oral dosage form of  claim 12 , wherein the opioid agonist is morphine sulfate and the ratio of said naltrexone to said morphine is from about 0.018:1 to about 1.148:1 by weight.  
     
     
         20 . The oral dosage form of  claim 12 , wherein the opioid agonist is oxycodone hydrochloride and the ratio of said naltrexone to said oxycodone is from about 0.037:1 to about 0.296:1 by weight.  
     
     
         21 . The oral dosage form of  claim 12 , wherein the opioid agonist is oxycodone hydrochloride and the ratio of said naltrexone to said oxycodone is from about 0.056:1 to about 0.222:1 by weight.  
     
     
         22 . The oral dosage form of  claim 12 , wherein the opioid agonist is hydrocodone bitartrate and the ratio of said naltrexone to said hydrocodone is from about 0.03:1 to about 0.27:1 by weight.  
     
     
         23 . The oral dosage form of  claim 12 , further comprising a sustained release carrier, wherein the sustained release carrier provides for a release of said opioid agonist such that the dosage form is suitable for administration on a twice-a-day or a once-a-day basis.