Solid dosage formulations of narcotic drugs having improved buccal adsorption

Abstract

The present invention provides solid dosage formulations of narcotic drugs with improved buccal adsorption. These improved characteristics are provided by the combination of the narcotic drug with an additional non-toxic soluble organic compound. The soluble organic compound contains a primary, secondary or tertiary amine group. The addition of this organic compound favorably alters the kinetics of mucosal penetration such that mucosal penetration times are decreased. This provides for a faster onset of action of the drug.

1 . Solid dosage formulations of narcotic drugs in form of buccal tablets characterized by containing a non toxic amine.  
   
   
       2 . Formulations according to  claim 1 , wherein the non-toxic amine is selected from Histidine, Arginine, Lysine, Triethanolamine, Trimethylamine, Betaine, Pyrrolidine, Guanidine, Cysteamine, Taurine and derivatives and analogues thereof.  
   
   
       3 . Formulations according to  claim 2  wherein the non-toxic amine is arginine.  
   
   
       4 . Formulations according to  claim 1  wherein the non-toxic amine is present in amounts ranging between 0.1 to 500% of the moles of active component(s), more preferably 0.5 to 300% and most preferably 1 to 200%.  
   
   
       5 . Formulations according to  claim 1  wherein the narcotic drug is selected from Alfentanil, Buprenorphine, Butorphanol, Codeine, Diphenoxylate, Fentanyl, Heroin, Hydrocodone, Hydromorphone, Oxymorphone, Levophanol, Levallorphan, Loperamide, Meperidine, Morfine, Nalbuphine, Nalmefene, Nalorphine, Naloxone, Naltrexone, Remifentanyl, Sufentanil.  
   
   
       6 . Formulations according to  claim 5  wherein the active ingredient is Fentanyl.