Oral pharmaceutical dispersion compositions

Abstract

The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic.

1 . An oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic. 
     
     
         2 . A composition as claimed in  claim 1  wherein said carrier is an aqueous gel. 
     
     
         3 . A composition as claimed in either of  claims 1  and  2  wherein said drug substance is an NSAID. 
     
     
         4 . A composition as claimed in  claim 3  wherein said drug substance is ibuprofen. 
     
     
         5 . A composition as claimed in  claim 4  wherein the pH of said carrier is in the range 4 to 4.5. 
     
     
         6 . An oral pharmaceutical composition comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion, wherein said drug substance is a hydrophilic drug dispersed in the lipid phase or a lipophilic drug substance dispersed in a, preferably continuous, aqueous phase of the emulsion. 
     
     
         7 . A pharmaceutical composition, comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion, wherein said drug substance is a hydrophilic drug dispersed in an oil phase and/or a lipophilic drug dispersed in a, preferably continuous, aqueous phase of the emulsion for use in medicine. 
     
     
         8 . A pharmaceutical composition, comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion, wherein said drug substance is a hydrophilic drug dispersed in an oil phase and/or a lipophilic drug dispersed in a, preferably continuous, aqueous phase of the emulsion, for use treatment of retroviral infection, tuberculosis, pneumonia, malaria, leprosy, erectile dysfunction, cancer, cardiovascular diseases, hypertension, pain, bacterial infection, vitamin deficiency or inflammation. 
     
     
         9 . A lipophilic drug substance having a functional electrostatic group having a pKa of 2 to 10 for use in a method of treatment of a human or non human animal subject to combat a condition responsive thereto, which method comprises orally administering to said subject an oral pharmaceutical composition comprising said drug substance dispersed in an aqueous carrier having a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic. 
     
     
         10 . The use of a lipophilic drug substance having a functional electrostatic group having a pKa of 2 to 10 for the manufacture of an oral pharmaceutical composition for use by oral administration in a method of treatment of a human or nonhuman animal subject to combat a condition responsive to said drug substance, said composition comprising said drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic. 
     
     
         11 . A method of treatment of a human or nonhuman animal subject by oral administration thereto of an effective amount of an oral pharmaceutical composition comprising a lipophilic drug substance having a functional electrostatic group having a pKa of 2 to 10 to combat a condition responsive to said drug substance, said composition comprising said drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic. 
     
     
         12 . Use of a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion for the manufacture of a medicament for use by oral administration in the treatment of retroviral infection, tuberculosis, pneumonia, malaria, leprosy, erectile dysfunction, cancer, cardiovascular diseases, hypertension, pain, bacterial infection, vitamin deficiency or inflammation, wherein said drug substance is a hydrophilic drug dispersed in an oil phase and/or a lipophilic drug dispersed in a, preferably continuous, aqueous phase of the emulsion. 
     
     
         13 . A method of treatment of a human subject to combat retroviral infection, tuberculosis, pneumonia, malaria, leprosy, erectile dysfunction, cancer, cardiovascular diseases, hypertension, pain, bacterial infection, vitamin deficiency or inflammation, which method comprises orally administering to said subject an effective amount of a pharmaceutical composition, comprising a drug substance contained in a physiologically tolerable gelled oil-in-water emulsion, wherein said drug substance is a hydrophilic drug dispersed in an oil phase and/or a lipophilic drug dispersed in a, preferably continuous, aqueous phase of the emulsion.