Pharmaceutical composition

Abstract

A pharmaceutical composition comprising: (A) a continuous liquid phase; (B) liquid droplets dispersed in said continuous phase; (C) a pharmaceutically-active compound; (D) an enhancer as described in U.S. Pat. No. 5,023,252; and (E) a hydrocolloid emulsifying agent; including, for example, a composition in which the liquid phase comprises an aqueous solution of insulin and the liquid droplets comprise a solution of the enhancer and a solvent therefore; and the use of the composition to treat a condition for example diabetes in a patient by applying to the membrane of the patient the composition.

1 . A pharmaceutical composition in the form of an emulsion and comprising: (A) a continuous liquid phase; (B) liquid droplets dispersed in said liquid phase; (C) a pharmaceutically-active compound; (D) a Hsieh enhancer; and (E) a hydrocolloid emulsifying agent;  
     
     
         2 . A composition according to  claim 1  in which the liquid phase comprises an aqueous solution of the pharmaceutically-active compound and the liquid droplets comprise a solution of the Hsieh enhancer and a solvent therefor.  
     
     
         3 . A composition according to  claim 1  in which the liquid phase comprises water and the liquid droplets comprise a solution of the pharmaceutically-active compound and the Hsieh enhancer and a solvent therefor.  
     
     
         4 . A composition according to  claim 1  which includes a hydrocolloid emulsifying agent that has an alkyl group containing from about 10 to about 50 carbon atoms.  
     
     
         5 . A composition according to  claim 2  which includes a hydrocolloid emulsifying agent that has an alkyl group containing from about 10 to about 50 carbon atoms.  
     
     
         6 . A composition according to  claim 4  which includes a hydrocolloid emulsifying agent that is an acrylates/C 10-30  alkyl acrylates crosspolymer.  
     
     
         7 . A composition according to  claim 5  which includes a hydrocolloid emulsifying agent that is an acrylates/C 10-30  alkyl acrylates crosspolymer.  
     
     
         8 . A composition according to  claim 3  which includes a hydrocolloid emulsifying agent which has an alkyl group containing from about 10 to about 50 carbon atoms.  
     
     
         9 . A composition according to  claim 8  which includes a hydrocolloid emulsifying agent that is an acrylates/C 10-30  alkyl acrylates crosspolymer.  
     
     
         10 . A composition according to  claim 2  in which the pharmaceutically-active compound is insulin.  
     
     
         11 . A composition according to  claim 2  in which the pharmaceutically-active compound is a water-soluble peptide.  
     
     
         12 . A composition according to  claim 2  in which the pharmaceutically-active compound is a precursor, congener, salt, complex, analog, or derivative of insulin.  
     
     
         13 . A composition according to  claim 10  in which the insulin is human recombinant insulin.  
     
     
         14 . A composition according to  claim 1  in which the enhancer is a macrocyclic enhancer.  
     
     
         15 . A composition according to  claim 14  in which the enhancer is a cyclic ester.  
     
     
         16 . A composition according to  claim 14  in which the enhancer is a pentadecalactone.  
     
     
         17 . A composition according to  claim 16  in which the enhancer is oxacycloheaxdecan-2-one.  
     
     
         18 . A composition according to  claim 2  in which the pharmaceutically-active compound is insulin, the enhancer is oxacyclohexadecan-2-one, and the emulsifying agent is an acrylates/C 10-30  alkyl acrylate crosspolymer.  
     
     
         19 . A composition according to  claim 18  in which the insulin is human recombinant insulin.  
     
     
         20 . A composition according to  claim 2  in which the pharmaceutically-active compound is a precursor, congener, salt, complex, analog, or derivative of insulin, the enhancer is oxacyclohexadecan-2-one, and the emulsifying agent is an acrylates/C 10-30  alkyl acrylate crosspolymer.  
     
     
         21 . A composition according to  claim 3  in which the pharmaceutically-active compound is an opiate alkaloid.  
     
     
         22 . A composition according to  claim 3  in which the pharmaceutically-active compound is oxycodone.  
     
     
         23 . A composition according to  claim 3  in which the pharmaceutically-active compound is oxycodone, the enhancer is oxacyclohexadecan-2-one, and the emulsifying agent is an acrylates/C 10-30  alkyl acrylate crosspolymer.  
     
     
         24 . A method for treating a condition in a patient comprising the step of delivering to a membrane of the patient a pharmaceutical composition comprising the composition of  claim 1 .  
     
     
         25 . A method for treating a patient who has diabetes comprising the step of spraying into the nostrils of the patient a pharmaceutical composition comprising the composition of  claim 10 .  
     
     
         26 . A method for treating a patient who has diabetes comprising the steps of spraying into the nostrils of the patient a pharmaceutical composition comprising the composition of  claim 12 .  
     
     
         27 . A method for treating a condition in a patient comprising the step of dropping or spraying into the eye or the sac of the eye of the patient a pharmaceutical composition according to  claim 2.