Pharmaceutical composition containing nicotinic acid and/or nicotinamide and/or tryptophan for positively influencing the intestinal microbiota

Abstract

The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.

1 - 21 . (canceled) 
     
     
         22 . A composition for positively influencing intestinal microbiota, comprising an active substance selected from the group consisting of nicotinic acid, nicotinamide, tryptophan, nicotinic acid esters, nicotinamide adenine dinucleotide (NAD), nicotinamide adenine dinucleotide phosphate (NADP), an intermediate in the biosynthesis of NAD or NADP selected from the group consisting of N-formylkynurenine, L-kynurenine, 3-hydroxy-L-kynurenine, 3-hydroxyanthranilate, 2-amino-3-carboxymuconate semialdehyde, quinolinate, and beta-nicotinate D-ribonucleotide, a tryptophan dipeptide, or a combination of two or more thereof; formulated for oral administration; and formulated for selective release in the terminal ileum, the colon, or both, for topical efficacy in the terminal ileum, the colon, or both, where the intestinal microbiota to be influenced are located to thereby positively influence the intestinal microbiota;
 wherein the composition is provided with a coating.   
     
     
         23 . The composition according to  claim 22 , wherein the selective release is achieved by the coating. 
     
     
         24 . The composition according to  claim 22 , wherein the coating is a film coating and/or is resistant to gastric juice and dissolves depending on the pH. 
     
     
         25 . The composition according to  claim 22 , wherein the composition comprises an active substance selected from the group consisting of nicotinic acid, nicotinamide, tryptophan, tryptophan dipeptide, and combinations of two or more thereof. 
     
     
         26 . The composition according to  claim 22 , wherein the composition comprises nicotinamide as an active substance. 
     
     
         27 . The composition according to  claim 22 , wherein the composition comprises (i) nicotinic acid and/or nicotinamide and (ii) acetylsalicylic acid as active substances. 
     
     
         28 . The composition according to  claim 22 , wherein the composition comprises tryptophan dipeptide as an active substance. 
     
     
         29 . The composition according to  claim 22 , further comprising a prostaglandin D2 antagonist. 
     
     
         30 . The composition according to  claim 22 , wherein the composition is further formulated to provide delayed release of the active substance(s) for specific local effect in the terminal ileum and/or colon. 
     
     
         31 . The composition according to  claim 30 , wherein the delayed release is achieved by the coating. 
     
     
         32 . The composition according to  claim 22 , wherein the composition is further formulated to provide controlled release of the active substance(s) for specific local effect in in the terminal ileum and/or colon. 
     
     
         33 . The composition according to  claim 32 , wherein the controlled release is achieved by the coating. 
     
     
         34 . A method comprising orally administering a composition according to  claim 22  to a human or animal in need thereof. 
     
     
         35 . The method of  claim 34 , wherein the method is for the therapy of or to reduce the likelihood of developing one or more conditions selected from the group consisting of inflammatory bowel disease, inflammatory diseases of the small intestine, diseases of the large intestine, colon carcinoma, and diseases of other body organs which result from changes in the intestinal microbiota and/or an impaired interaction between intestinal microbiota and intestines. 
     
     
         36 . The method of  claim 34 , wherein the method is for the therapy of or to reduce the likelihood of developing inflammatory bowel disease. 
     
     
         37 . The method of  claim 36 , wherein the inflammatory bowel disease is ulcerative colitis or Crohn's disease. 
     
     
         38 . The method of  claim 34 , wherein the method is for positively influencing the intestinal microbiota. 
     
     
         39 . The method of  claim 34 , wherein the composition is further formulated to provide controlled and/or delayed release of the active substance(s) for specific local effect in the terminal ileum and/or colon, wherein the method provides controlled and/or delayed release of the active substance(s). 
     
     
         40 . The method of  claim 34 , wherein the composition further comprises a prostaglandin D2 antagonist. 
     
     
         41 . A composition for positively influencing intestinal microbiota, comprising an active substance selected from the group consisting of nicotinic acid, nicotinamide, tryptophan, nicotinic acid esters, nicotinamide adenine dinucleotide (NAD), nicotinamide adenine dinucleotide phosphate (NADP), an intermediate in the biosynthesis of NAD or NADP selected from the group consisting of N-formylkynurenine, L-kynurenine, 3-hydroxy-L-kynurenine, 3-hydroxyanthranilate, 2-amino-3-carboxymuconate semialdehyde, quinolinate, and beta-nicotinate D-ribonucleotide, a tryptophan dipeptide, or a combination of two or more thereof; formulated for rectal administration or neorectal administration; and formulated for selective release in the terminal ileum, the colon, or both, for topical efficacy in the terminal ileum, the colon, or both, where the intestinal microbiota to be influenced are located to thereby positively influence the intestinal microbiota;
 wherein the composition is provided with a coating.   
     
     
         42 . A method comprising rectally administering or neorectally administering a composition according to  claim 41  to a human or animal in need thereof. 
     
     
         43 . The method of  claim 42 , wherein the method is for the therapy of or to reduce the likelihood of developing one or more conditions selected from the group consisting of inflammatory bowel disease, inflammatory diseases of the small intestine, diseases of the large intestine, colon carcinoma, and diseases of other body organs which result from changes in the intestinal microbiota and/or an impaired interaction between intestinal microbiota and intestines. 
     
     
         44 . The method of  claim 43 , wherein the method is for the therapy of or to reduce the likelihood of developing inflammatory bowel disease. 
     
     
         45 . The method of  claim 42 , wherein the method is for positively influencing the intestinal microbiota.