Buccal, polar and non-polar spray or capsule containing drugs for treating pain

Abstract

Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

1 - 55 . (canceled) 
     
     
         56 . A method of treating pain in a human patient comprising:
 providing an oral spray composition comprising fentanyl or a pharmaceutically acceptable salt thereof in an amount between 0.001 and 60 percent by weight of the total composition; and   a polar solvent in an amount between 30 and 99.69 percent by weight of the total composition; and   spraying the composition on the oral mucosa of the patient to provide transmucosal absorption of an amount of fentanyl through the oral mucosa of the patient sufficient to treat the patient's pain.   
     
     
         57 . The method of  claim 56 , the composition further comprising a flavoring agent in an amount between 0.1 and 10 percent by weight of the total composition. 
     
     
         58 . The method of  claim 57 , wherein the polar solvent is present in an amount between 37 and 98.58 percent by weight of the total composition, fentanyl or a pharmaceutically acceptable salt thereof is present in an amount between 0.005 and 55 percent by weight of the total composition, and the flavoring agent is present in an amount between 0.5 and 8 percent by weight of the total composition. 
     
     
         59 . The method of  claim 57 , wherein the polar solvent is present in an amount between 60.9 and 97.06 percent by weight of the total composition, fentanyl or a pharmaceutically acceptable salt thereof is present in an amount between 0.01 and 40 percent by weight of the total composition, and the flavoring agent is present in an amount between 0.75 and 7.5 percent by weight of the total composition. 
     
     
         60 . The method of  claim 56 , wherein the polar solvent comprises a polyethylene glycol having a molecular weight between 400 and 1000, a C 2  to C 8  mono- and polyalcohol, or a C 7  to C 18  alcohol of linear or branched configuration. 
     
     
         61 . The method of  claim 56 , wherein the polar solvent comprises aqueous polyethylene glycol. 
     
     
         62 . The method of  claim 56 , wherein the polar solvent comprises aqueous ethanol. 
     
     
         63 . A method of treating pain in a human patient comprising:
 providing an oral spray composition comprising fentanyl or a pharmaceutically acceptable salt thereof in an amount between 0.005 and 55 percent by weight of the total composition; and   a non-polar solvent in an amount between 30 and 99.69 percent by weight of the total composition; and   spraying the composition on the oral mucosa of the patient to provide transmucosal absorption of an amount of fentanyl through the oral mucosa of the patient sufficient to treat the patient's pain.   
     
     
         64 . The method of  claim 63 , the composition further comprising a flavoring agent in an amount between 0.1 and 10 percent by weight of the total composition. 
     
     
         65 . The method of  claim 63 , wherein the solvent comprises a (C 2 -C 24 ) fatty acid (C 2 -C 6 ) ester, a C 7 -C 18  hydrocarbon of linear or branched configuration, a C 2 -C 6  alkanoyl ester, or a triglyceride of C 2 -C 6  carboxylic acid. 
     
     
         66 . The method of  claim 65 , wherein the solvent comprises one or more fatty acid esters.