Buccal, polar and non-polar spray of capsule

Abstract

Buccal aerosol sprays or capsule 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 comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.

1 . A buccal polar pump spray composition for transmucosal administration of a pharmacologically active compound soluble in a pharmacologically acceptable polar solvent said composition comprising in weight % of total composition: polar solvent 37-98.58%, active compound 0.005-55% 
 wherein the active compound is selected from the group consisting of biologically active peptides, central nervous system active amines, sulfonyl ureas, antibiotics, antifungals, antivirals, sleep inducers, antiasthmatics, antiemetics, histamine H-2 receptor antagonists, barbiturates, prostoglandins, bronchial dilators selected from the group consisting of terbutaline, and theophylline.    
     
     
         2 . The composition of  claim 1  additionally comprising, by weight of total composition: flavoring agent 0.1-10%.  
     
     
         3 . The composition of  claim 1  comprising: polar solvent 60.9-97.06%, active compound 0.01-40%, flavoring agent 0.75-7.5%.  
     
     
         4 . The composition of  claim 1  wherein the polar solvent is selected from the group consisting of low molecular weight polyethylene-glycols (PEG) of 400-1000 MW, C 2 -C 8  mono- and poly-alcohols, and alcohols of C 7 -C 18  hydrocarbons of a linear or branched configuration.  
     
     
         5 . The composition of  claim 1  wherein the solvent is aqueous polyethylene glycol.  
     
     
         6 . The composition of  claim 1  wherein the solvent comprises aqueous ethanol.  
     
     
         7 . The composition of  claim 1  wherein the active compound is selected from the group consisting of cyclosporin, clozapine, zidevudine, erythromycin, odansetron, cimetidine, phenytoin, carboprost thromethamine, and valerian in their nonionized form or as the pharmaceutically acceptable salts thereof.  
     
     
         8 . The composition of  claim 2  wherein the flavoring agents are selected from the group consisting of synthetic or natural oil of peppermint, oil of spearmint, citrus oil, fruit flavors, sweeteners and combinations thereof.  
     
     
         9 . The composition of  claim 2  of the formulation: polar solvent 75-85%, cyclosporin 15-25%, flavoring agent 0.1-5%.  
     
     
         10 . The composition of  claim 2  of the formulation: polar solvent 19-90%, odansitron hydrochloride 2.5-15%, flavoring agent 1-10%.  
     
     
         12 . A method of administering a pharmacologically active compound to a mammal in needed of same, by spraying the oral mucosa of said mammal with a composition of  claim 1 .  
     
     
         13 . The method of  claim 12  wherein the amount of spray administered is predetermined.