Formulations Containing Expectorants or Decongestants

Abstract

The present invention relates to bioavailable fill compositions containing one or more of a decongestant, an expectorant, an antitussive, an analgesic, and/or an antihistamine; capsules filled with the bioavailable fill compositions; and methods of making same.

1 . A clear bioavailable liquid composition comprising:
 (a) two or more active ingredients selected from the group consisting of:
 acetaminophen, 
 guaifenesin, 
 phenylephrine and/or a pharmaceutically acceptable salt thereof, 
 dextromethorphan and/or a pharmaceutically acceptable salt thereof, 
 diphenhydramine and/or a pharmaceutically acceptable salt thereof, and 
 pseudoephedrine and/or a pharmaceutically acceptable salt thereof; 
   (b) a matrix comprising:
 1. 20-70 wt % of a pharmaceutically acceptable poly(alkylene glycol), and 
 2. 0.5-8 wt % of a pharmaceutically acceptable alkylene glycol; and 
   (c) a solubilizing agent comprising:
 1-30 wt % of a pharmaceutically acceptable polymeric solubilizing agent, and 
 1-10 wt % by weight water; 
   wherein said wt % values are based on the total weight of the composition, and wherein said fill composition is clear.   
     
     
         2 . The clear bioavailable liquid composition of  claim 1 , wherein the matrix comprises:
 40-60 wt % of a pharmaceutically acceptable poly(alkylene glycol), and   1-6 wt % of a pharmaceutically acceptable alkylene glycol.   
     
     
         3 . (canceled) 
     
     
         4 . The clear bioavailable liquid composition of  claim 1 , wherein the solubilizing agent comprises:
 4-20 wt % of a pharmaceutically acceptable polymeric solubilizing agent, and   5-10 wt % by weight water.   
     
     
         5 . (canceled) 
     
     
         6 . The clear bioavailable liquid composition of  claim 1 , comprising:
 0 to about 30.0 wt % acetaminophen,   0 to about 25.0 wt % guaifenesin,   0 to about 1.0 wt % phenylephrine HCl.   0 to about 2.0 wt % dextromethorphan HBr,   0 to about 3.0 wt % diphenhydramine HCl, or   0 to about 5.0 wt % pseudoephedrine HCl;   
       provided that at least two active ingredients are present in >0 wt %. 
     
     
         7 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 22.0 to about 25.0 wt % guaifenesin and   about 0.5 to 0.7 wt % phenylephrine HCl.   
     
     
         8 . The clear bioavailable liquid composition of  claim 7 , wherein the composition is about 860 mg comprising:
 about 200 mg guaifenesin,   about 5.13 mg phenylephrine HCl,   about 404.87 mg polyethylene glycol 400,   about 20 mg propylene glycol,   about 150 mg Povidone (k12), and   about 80 mg water.   
     
     
         9 . (canceled) 
     
     
         10 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 22.0 to about 25.0 wt % guaifenesin and   about 1.0 to 2.0 wt % dextromethorphan HBr (95%).   
     
     
         11 . The clear bioavailable liquid composition of  claim 10 , wherein the composition is about 865 mg comprising:
 about 200 mg guaifenesin,   about 10.526 mg dextromethorphan HBR (95%),   about 404.474 mg polyethylene glycol 400,   about 20 mg propylene glycol,   about 150 mg Povidone (k12), and   about 80 mg water.   
     
     
         12 . (canceled) 
     
     
         13 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 21.0 to about 24.0 wt % guaifenesin,   about 0.40 to about 1.0 wt % phenylephrine HCl, and   about 1.0 to 2.0 wt % dextromethorphan HBr (95%).   
     
     
         14 . The clear bioavailable liquid composition of  claim 13 , wherein the composition is about 885 mg comprising:
 about 200 mg guaifenesin,   about 5.25 mg phenylephrine HCl,   about 10.526 mg dextromethorphan HBr (95%),   about 419.224 mg polyethylene glycol 400,   about 20 mg propylene glycol,   about 150 mg Povidone (k12), and   about 80 mg water.   
     
     
         15 . (canceled) 
     
     
         16 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 21.0 to about 24.0 wt % acetaminophen,   about 13.0 to about 16.0 wt % guaifenesin, and   about 0.2 to about 0.6 wt % phenylephrine HCl.   
     
     
         17 . The clear bioavailable liquid composition of  claim 16 , wherein the composition is about 1415 mg comprising:
 about 325 mg acetaminophen,   about 200 mg guaifenesin,   about 5.25 mg phenylephrine HCl,   about 671.75 mg polyethylene glycol 400,   about 28 mg propylene glycol,   about 100 mg Povidone (k12), and   about 85 mg water.   
     
     
         18 . (canceled) 
     
     
         19 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 25.0 to about 28.0 wt % acetaminophen,   about 0.30 to about 0.60 wt % phenylephrine HCl, and   about 1.0 to about 3.0 wt % diphenhydramine HCl.   
     
     
         20 . The clear bioavailable liquid composition of  claim 19 , wherein the composition is about 1240 mg comprising:
 about 325 mg acetaminophen,   about 5.25 mg phenylephrine HCl,   about 25 mg diphenhydramine HCl,   about 684.75 mg polyethylene glycol 400,   about 50 mg propylene glycol,   about 65 mg Povidone (k30), and   about 85 mg water.   
     
     
         21 . (canceled) 
     
     
         22 . The clear bioavailable liquid composition of  claim 1 , comprising the following as the only active ingredients:
 about 21.0 to about 25.0 wt % guaifenesin and   about 2 to 5 wt % pseudoephedrine HCl.   
     
     
         23 . The clear bioavailable liquid composition of  claim 22 , wherein the composition is about 850-890 mg comprising:
 about 200 mg guaifenesin and   about 30 mg pseudoephedrine HCl.   
     
     
         24 . The clear bioavailable liquid composition of  claim 1 , comprising only two or three active ingredients selected from the group (a). 
     
     
         25 . The clear bioavailable liquid composition of  claim 24 , wherein said two or three active ingredients are the only active ingredients. 
     
     
         26 . A pharmaceutical composition in the form of a soft gelatin capsule of a size suitable for easy swallowing and typically containing from about 100 mg to about 2000 mg of a solubilized pharmaceutical active composition, comprising:
 (a) an outer gelatin shell; and   (b) a safe and effective mount of the clear bioavailable liquid composition of  claim 1  which is encapsulated by said outer gelatin shell.   
     
     
         27 . A pharmaceutical composition in the form of a soft gelatin capsule of a size suitable for easy swallowing and typically containing from about 100 mg to about 2000 mg of a solubilized pharmaceutical active composition, comprising:
 (a) an outer gelatin shell; and   (b) a safe and effective mount of the clear bioavailable liquid composition of  claim 6  which is encapsulated by said outer gelatin shell.