Chemotherapeutic compositions

Abstract

The present invention relates to the treatment of gastrointestinal and/or cancer, and a method of weight gain, via the ingestion of polymeric compositions in humans, animals or birds in need of said treatment. The invention provides methods for the treatment of cancer, the treatment and/or prevention of gastrointestinal disease and/or infection and/or diarrhea, and a method for increasing weight gain in humans, animals or birds comprising administering to said humans, animals or birds an effective amount of a pharmaceutical or veterinary composition, or feed additive, comprising an effective amount of a polymer and/or copolymer, having the repeating polymeric unit (I), wherein R is H or alkyl, usually C 1 to C 4 , or this unit in hydrated, hemiacetal or acetal form, together with a pharmaceutically or veterinarally acceptable carrier, diluent, adjuvant, excipient and/or controlled release system.

1 . A composition for treatment of gastrointestinal disease wherein said composition comprises:
 (a) a chemotherapeutic active compound comprising a polymer and/or copolymer of acrolein, having a structure according to Formula I:   
     
       
         
         
             
             
         
       
        as the repeating polymeric unit, wherein R is H or alkyl, preferably C 1  to C 4  or this unit in hydrated, hemiacetal or acetal form; and 
       (b) a pharmaceutically or veterinarally acceptable carrier. 
     
   
   
       2 . The composition according to  claim 1  in the form of pellets comprising a controlled release system of a crosslinked water absorbent polymer matrix adapted to form a gel when wet. 
   
   
       3 . The composition according to  claim 1  wherein the carrier is selected from the group consisting of polymers and copolymers of one or more of acrylic acid, methacrylic acid, esters of acrylic acid, esters of methacrylic acid, amides of acrylic acid and amides of methacrylic acid, polyvinyl alcohol and polyvinyl acetate. 
   
   
       4 . The composition according to  claim 1  wherein the carrier is selected from the group consisting of polymers and copolymers of one or more of acrylic acid, methacrylic acid, esters of acrylic acid, esters of methacrylic acid, amides of acrylic acid and amides of methacrylic acid, polyvinyl alcohol and polyvinyl acetate. 
   
   
       5 . The composition according to  claim 1  wherein the carrier comprises a polymer of acrylic acid and/or a copolymer of acrylic acid and acrylamide. 
   
   
       6 . The composition according to  claim 1  wherein the active agent is present in an amount of from 5 to 50% by weight of the composition. 
   
   
       7 . The composition according to  claim 1  comprising a liquid carrier selected from the group consisting of water, olive oil, peanut oil, sesame oil, sunflower oil, arachis oil, coconut oil, liquid paraffin, ethylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol, ethanol, propanol, isopropanol, glycerol, fatty alcohols, triglycerides and mixtures thereof. 
   
   
       8 . The composition according to  claim 1  wherein the liquid carrier is selected from the group consisting of ethylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol, ethanol propanols, isopropanols, glycerol, fatty alcohols, triglycerides and mixtures thereof. 
   
   
       9 . The composition according to  claim 1  wherein the carrier comprises polyethylene glycol and water. 
   
   
       10 . The composition according to  claim 1  wherein the carrier comprises controlled release pellets wherein said pellets are added to animal feed to provide a feed containing from 1% to 20% by weight of said polymer or copolymer of acrolein. 
   
   
       11 . The composition according to  claim 1  wherein said polymer or copolymer of acrolein has a molecular weight greater than 1000 Daltons. 
   
   
       12 . The composition according  claim 1  wherein the polymer or copolymer of acrolein comprises in the range from 0.1 to 5 moles of carboxyl groups per kilogram of said polymer or copolymer of acrolein. 
   
   
       13 . The composition according to  claim 1  wherein the repeating polymeric unit is in the hydrated diol form, the hemiacetal or acetal form, as formed from the condensation of diol form with the aldehyde or diol form, the tetrahydropyran or fused tetrahydropyran formed from condensation of the diol form, the aldol-Michael self-condensation form or mixtures thereof illustrated, non-comprehensively by the following formulae: 
     
       
         
         
             
             
         
       
     
     wherein n is one or more. 
   
   
       14 . A chemotherapeutic composition in the form of pellets comprising:
 (a) an active agent comprising polymers and/or copolymers of acrolein having the repeating polymeric unit:   
     
       
         
         
             
             
         
       
        wherein R is H or alkyl, preferably C 1  to C 4 , or this unit is hydrated, hemiacetal or acetal form, together with a pharmaceutically or veterinarally acceptable carrier, and 
       (b) a polymeric matrix within which the active agent is contained; and 
        wherein the pellets are formed by a process comprising the step of adding a polymeric matrix to a solution and/or suspension and/or emulsion of said polymers and/or copolymers. 
     
   
   
       15 . The chemotherapeutic composition according to  claim 14 , wherein adding said polymeric matrix to a solution and/or suspension and/or emulsion of the said polymers and/or copolymers, comprises the steps of:
 (i) dissolving said polymers or copolymers in an aqueous alkaline or basic solution;   (ii) neutralising said solution with acid;   (iii) adding to said neutralised solution insoluble, crosslinked, absorbent polymers of acrylic acid and/or copolymers of acrylamide and acrylic acid to form wet swollen pellets.   
   
   
       16 . The chemotherapeutic composition according to  claim 14  wherein the wet, swollen pellets are at least partly dried. 
   
   
       17 . A method of treatment or prevention of a gastrointestinal dysfunction in a human, animal or bird comprising administering to said human, animal or bird the composition according to  claim 1 . 
   
   
       18 . The method according to  claim 17  wherein the polymer or copolymer comprises carboxyl groups at a concentration of from 0.1 to 5 moles of carboxyl groups per kilogram of polymer. 
   
   
       19 . The method according to  claim 17  wherein the gastrointestinal dysfunction is a gastrointestinal disease, gastrointestinal infection or diarrhea resulting from an infection of the gastrointestinal tract. 
   
   
       20 . The method according to  claim 17  wherein the gastrointestinal dysfunction is a bacterial disease or infection or cancer.