Oral liquid mucoadhesive compositions

Abstract

The present invention relates to a per oral, oral, or intranasal pharmaceutical mucoretentive, aqueous liquid composition comprising from about 2% to about 50%, by weight of the composition, of colloidal particles of silica, titanium dioxide, clay, and mixtures thereof and a safe and effective amount of a pharmaceutical active selected from the group consisting of analgesics, decongestants, expectorants, antitussives, antihistamines, sensory agents, gastrointestinal agents, and mixtures thereof; wherein the composition has a sedimentation volume ratio of greater than about 0.90 and wherein the triggered viscosity ratio of the composition is at least about 1.2. The present invention further relates to a method of coating the alimentary canal and nasal mucosa, in particular to a method of preventing or treating symptoms of upper respiratory tract infections or upper respiratory tract tissue irritation or damage, by administering a safe and effective amount of the above composition.

What is claimed is:  
     
         1 . A per oral or oral, mucoretentive, aqueous liquid, pharmaceutical composition comprising: 
 (a) from about 2% to about 50%, by weight of the composition, of colloidal particles of silica; and    (b) a safe and effective amount of a pharmaceutical active selected from the group consisting of gastrointestinal agents, analgesics, decongestants, expectorants, antitussives, antihistamines, bronchodilators, topical anesthetics, sensory agents, oral care agents, miscellaneous respiratory agents, and mixtures thereof;    wherein the composition has a sedimentation volume ratio of greater than about 0.90 when measured after about 48 hours, and a triggered viscosity ratio of at least about 1.2.    
     
     
         2 . The composition of  claim 1  wherein the composition is not further diluted with any liquid prior to administration and the level of silica is from about 3% to about 15%, by weight of the composition.  
     
     
         3 . The composition of  claim 1  wherein the composition has a sedimentation volume ratio of greater than about 0.95, when measured after about 48 hours.  
     
     
         4 . The composition of  claim 3  wherein the composition has a sedimentation volume ratio of greater than about 0.98, when measured after about 48 hours.  
     
     
         5 . The composition of  claim 1  wherein the composition has a triggered viscosity ratio of at least about 1.4.  
     
     
         6 . The composition of  claim 5  wherein the composition has a triggered viscosity ratio of at least about 1.5.  
     
     
         7 . The composition of  claim 6  wherein the silica has a mean particle size of less than about 1 micron.  
     
     
         8 . The composition of  claim 1  wherein the composition has a zero shear viscosity of greater than about 2,000 pascal seconds.  
     
     
         9 . The composition of  claim 8  wherein the composition has a zero shear viscosity of greater than about 7,500 pascal seconds.  
     
     
         10 . The composition of  claim 7  wherein the silica is silicon dioxide.  
     
     
         11 . The composition of  claim 10  wherein the silicon dioxide is selected from the group consisting of fumed silicon dioxide, precipitated silicon dioxide, coacervated silicon dioxide, and gel silicon dioxide.  
     
     
         12 . The composition of  claim 1  additionally comprising from 0.005% to 3% citric acid or salt thereof.  
     
     
         13 . An intranasal, mucoretentive, aqueous liquid pharmaceutical composition comprising: 
 (a) from about 2% to about 50%, by weight of the composition, of colloidal particles of silica; and    (b) a safe and effective amount of a pharmaceutical active selected from the group consisting of gastrointestinal agents, analgesics, decongestants, expectorants, antitussives, antihistamines, bronchodilators, topical anesthetics, sensory agents, oral care agents, miscellaneous respiratory agents, and mixtures thereof;    wherein the composition has a sedimentation volume ratio of greater than about 0.90 when measured after about 48 hours, and a triggered viscosity ratio of at least about 1.2.    
     
     
         14 . The composition of  claim 13  wherein the composition has a sedimentation volume ratio of greater than about 0.95 when measured after about 48 hours.  
     
     
         15 . The composition of  claim 14  wherein the composition has a sedimentation volume ratio of greater than about 0.98 when measured after about 48 hours.  
     
     
         16 . The composition of  claim 13  wherein the composition has a triggered viscosity ratio of at least about 1.4.  
     
     
         17 . The composition of  claim 16  wherein the composition has a triggered viscosity ratio of at least about 1.5.  
     
     
         18 . The composition of  claim 13  wherein the level of silica is from about 3% to about 15%, by weight of the composition.  
     
     
         19 . The composition of  claim 18  wherein the silica has a mean particle size of less than about 1 micron.  
     
     
         20 . The composition of  claim 13  wherein the composition has a zero shear viscosity of greater than about 2,000 pascal seconds.  
     
     
         21 . The composition of  claim 20  wherein the composition has a zero shear viscosity of greater than about 7,500 pascal seconds.  
     
     
         22 . The composition of  claim 19  wherein the silica is silicon dioxide.  
     
     
         23 . The composition of  claim 22  wherein the silicon dioxide is selected from the group consisting of fumed silicon dioxide, precipitated silicon dioxide, coacervated silicon dioxide, and gel silicon dioxide.  
     
     
         24 . A method of coating the alimentary canal by administering a safe and effective amount of the composition of  claim 1 .  
     
     
         25 . A method of coating the nasal mucosa by administering a safe and effective amount of the composition of  claim 13 .  
     
     
         26 . A method of preventing or treating symptoms of upper respiratory tract infections or upper respiratory tract tissue irritation or damage, by administering a safe and effective amount of the composition of  claim 1 .  
     
     
         27 . A method of preventing or treating symptoms of upper respiratory tract infections or upper respiratory tract tissue irritation or damage, by administering a safe and effective amount of the composition of  claim 13 .  
     
     
         28 . A method of administering an active agent to the alimentary canal, by administering a safe and effective amount of the composition of  claim 1 .  
     
     
         29 . A method of administering an active agent to the nasal mucosa, by administering a safe and effective amount of the composition of claim  13 .