Oral antimicrobial pharmaceutical compositions

Abstract

The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

1 . Oral pharmaceutical composition providing controlled release or delayed release of metronidazole as an active ingredient or both controlled and delayed release thereof, said composition containing metronidazole in association with one or more pharmacologically acceptable excipients(s), wherein the release is given by a multi-matrix structure comprising:
 a) an amphiphilic matrix in which the active ingredient is incorporated;   b) a lipophilic matrix which is formed by substances having a melting point of less than 90° C. and in which a) is dispersed; and   c) a hydrophilic matrix.   
     
     
         2 . Pharmaceutical composition according to  claim 1 , wherein the release of the active ingredient takes place in the large intestine. 
     
     
         3 . Pharmaceutical composition according to  claim 1 , wherein the release of the active ingredient takes place in the colon. 
     
     
         4 . Pharmaceutical composition according to  claim 1 , wherein the metronidazole is contained in an amount of from 10 to 90% by weight. 
     
     
         5 . Pharmaceutical composition according to  claim 4 , wherein the metronidazole is contained in an amount of from 25 to 70% by weight. 
     
     
         6 . Pharmaceutical composition according to  claim 1 , wherein the amphiphilic matrix is selected from at least one member of the group consisting of lecithin, polyoxyethylenated sorbitan monooleate, sodium lauryl sulphate, sodium dioctyl sulphosuccinate, ethylene and propylene block copolymers. 
     
     
         7 . Pharmaceutical composition according to  claim 1 , wherein the lipophilic matrix is selected from at least one member of the group consisting of stearic acid, beeswax, carnauba wax, palmitic acid and palmitostearate esters. 
     
     
         8 . Pharmaceutical composition according to  claim 1 , wherein the hydrophilic matrix is selected from at least one member of the group consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, carboxyvinyl polymers, polyvinyl alcohol, vinyl polymers, alginic acid and its salts and polysaccharide polymers. 
     
     
         9 . Pharmaceutical composition according to  claim 1 , comprising a gastro-protective coating. 
     
     
         10 . Pharmaceutical composition according to  claim 9 , wherein the gastro-protective coating is selected from at least one member of the group consisting of acrylic acid esters, methacrylic acid esters, and cellulose acetate phthalate. 
     
     
         11 . A method for treating a disorder selected from the group consisting of pathologies of the large intestine comprising administering to a subject in need of treatment a composition according to  claim 1 . 
     
     
         12 . A method for treating a disorder selected from the group consisting of pathologies of the colon comprising administering to a subject in need of treatment a composition according to  claim 1 . 
     
     
         13 . A method for treating a disorder selected from the group consisting of infectious colites, bacillary dysentery, pseudomembranous colitis, travellers' diarrhoea, diverticular disease, and diverticulitis comprising administering to a subject in need of treatment a composition according to  claim 1 . 
     
     
         14 . A method for treating a disorder selected from the group consisting of surgical operations on the colon and for support treatment in the therapy of ammonaemias or hyperammonaemias comprising administering to a subject in need of treatment a composition according to  claim 1 .