Buccal, polar and non-polar spray containing ondansetron

Abstract

Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron 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, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant.

1 - 104 . (canceled) 
   
   
       105 . A method of administering ondansetron to a mammal comprising spraying the oral mucosa of the mammal with a propellant free buccal spray composition to provide transmucosal absorption of a pharmacologically effective amount of ondansetron through the oral mucosa of the mammal to the systemic circulatory system of the mammal, the composition comprising:
 ondansetron or a pharmaceutically acceptable salt thereof in an amount of 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; wherein a pharmacologically effective amount of ondansetron is absorbed through the oral mucosa of the mammal to the mammal's systemic circulatory system.   
   
   
       106 . The method of  claim 105 , further comprising a taste mask and/or flavoring agent in an amount of between 0.1 and 10 percent by weight of the total composition. 
   
   
       107 . The method of  claim 106 , wherein the polar solvent is present in an amount between 37 and 98.58 percent by weight of the total composition, the ondansetron 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 taste mask and/or flavoring agent is present in an amount between 0.5 and 8 percent by weight of the total composition. 
   
   
       108 . The method of  claim 107 , wherein the polar solvent is present in an amount between 60.9 and 97.06 percent by weight of the total composition, the ondansetron 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 taste mask and/or flavoring agent is present in an amount between 0.75 and 7.5 percent by weight of the total composition. 
   
   
       109 . The method of  claim 105 , wherein the polar solvent is selected from the group consisting of polyethylene glycols having a molecular weight between 400 and 1000, C 2  to C 8  mono- and poly-alcohols, and C 7  to C 18  alcohols of linear or branched configuration. 
   
   
       110 . The method of  claim 105 , wherein the polar solvent comprises polyethylene glycol. 
   
   
       111 . The method of  claim 105 , wherein the polar solvent comprises ethanol. 
   
   
       112 . The method of  claim 106 , wherein the flavoring agent is selected from the group consisting of synthetic or natural oil of peppermint, oil of spearmint, citrus oil, fruit flavors, sweeteners, and mixtures thereof. 
   
   
       113 . The method of  claim 105 , wherein the amount of the spray is predetermined. 
   
   
       114 . A method of administering ondansetron to a mammal comprising spraying the oral mucosa of the mammal with a propellant free buccal spray composition to provide transmucosal absorption of a pharmacologically effective amount of ondansetron through the oral mucosa of the mammal to the systemic circulatory system of the mammal, the composition comprising:
 ondansetron 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; wherein a pharmacologically effective amount of ondansetron is absorbed through the oral mucosa of the mammal to the mammal's systemic circulatory system.   
   
   
       115 . The method of  claim 114 , further comprising a taste mask and/or flavoring agent in an amount between 0.1 and 10 percent by weight of the total composition. 
   
   
       116 . The method of  claim 115 , wherein the flavoring agent is selected from the group consisting of synthetic or natural oil of peppermint, oil of spearmint, citrus oil, fruit flavors, sweeteners, and mixtures thereof. 
   
   
       117 . The method of  claim 114 , wherein the solvent is selected from the group consisting of (C 2 -C 24 ) fatty acid (C 2 -C 6 ) esters, C 7 -C 18  hydrocarbons of linear or branched configuration, C 2 -C 6  alkanoyl esters, and triglycerides of C 2 -C 6  carboxylic acids. 
   
   
       118 . The method of  claim 117 , wherein the solvent is a triglyceride. 
   
   
       119 . The method of  claim 114 , wherein the amount of the spray is predetermined. 
   
   
       120 . A method of administering ondansetron to a mammal comprising spraying the oral mucosa of the mammal with a propellant free buccal spray composition to provide transmucosal absorption of a pharmacologically effective amount of ondansetron through the oral mucosa of the mammal to the systemic circulatory system of the mammal, the composition comprising:
 ondansetron or a pharmaceutically acceptable salt thereof in an amount of between 0.001 and 60 percent by weight of the total composition; and   a mixture of a polar solvent and a non-polar solvent in an amount of between 30 and 99.69 percent by weight of the total composition, wherein the ratio of the polar solvent to the non-polar solvent ranges from 1:99 to 99:1; wherein a pharmacologically effective amount of ondansetron is absorbed through the oral mucosa of the mammal to the mammal's systemic circulatory system.   
   
   
       121 . The method of  claim 120 , further comprising a taste mask and/or flavoring agent in an amount of between 0.1 and 10 percent by weight of the total composition. 
   
   
       122 . The method of  claim 121 , wherein the polar solvent is present in an amount between 37 and 98.58 percent by weight of the total composition, the ondansetron 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 taste mask and/or flavoring agent is present in an amount between 0.5 and 8 percent by weight of the total composition. 
   
   
       123 . The method of  claim 122 , wherein the polar solvent is present in an amount between 60.9 and 97.06 percent by weight of the total composition, the ondansetron 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 taste mask and/or flavoring agent is present in an amount between 0.75 and 7.5 percent by weight of the total composition. 
   
   
       124 . The method of  claim 120 , wherein the polar solvent is selected from the group consisting of polyethylene glycols having a molecular weight between 400 and 1000, C 2  to C 8  mono- and poly-alcohols, and C 7  to C 18  alcohols of linear or branched configuration and the non-polar solvent is selected from the group consisting of (C 2 -C 24 ) fatty acid (C 2 -C 6 ) esters, C 7 -C 18  hydrocarbons of linear or branched configuration, C 2 -C 6  alkanoyl esters, and triglycerides of C 2 -C 6  carboxylic acids. 
   
   
       125 . The method of  claim 121 , wherein the flavoring agent is selected from the group consisting of synthetic or natural oil of peppermint, oil of spearmint, citrus oil, fruit flavors, sweeteners, and mixtures thereof. 
   
   
       126 . The method of  claim 120 , wherein the amount of the spray is predetermined.