Formulations for a tight junction effector

Abstract

Enteric compositions comprising one or more tight junction agonists and/or one or more tight junction antagonists are provided. Compositions of the invention may comprise a delayed-release coating disposed over a tight junction agonist and/or tight junction antagonist layer which may be disposed over an inert core. Delayed-release coatings may be substantially stable in gastric fluid and substantially unstable in intestinal fluid, thus providing for substantial release of the tight junction agonist and/or antagonist from the composition in the duodenum or jejunum of the small intestine.

1 - 59 . (canceled) 
     
     
         60 . An oral dosage composition comprising an effective amount of Larazotide acetate (AT1001), wherein the composition comprises delayed-release particles comprising:
 a core particle;   a base coat comprising Larazotide acetate over the core particle; and   a delayed-release coating disposed over the base coat.   
     
     
         61 . The composition of  claim 60 , wherein the Larazotide acetate is about 0.1% to about 20% by weight of the composition. 
     
     
         62 . The composition of  claim 61 , wherein the Larazotide acetate is about 0.1% to about 6% by weight of the composition. 
     
     
         63 . The composition of  claim 60 , wherein the composition is in the form of a capsule or tablet. 
     
     
         64 . The composition of  claim 60 , wherein the core particle has an average size of from about 5 to about 50 mesh. 
     
     
         65 . The composition of  claim 64 , wherein the core particle has an average size of from about 15 to about 40 mesh. 
     
     
         66 . The composition of  claim 60 , the core particle comprises an oxide, cellulose, a polymer, an inorganic salt, or a sugar 
     
     
         67 . The composition of  claim 66 , wherein the core particle comprises a sugar. 
     
     
         68 . The composition of  claim 60 , wherein the delayed-release coating is substantially stable in an acidic environment and substantially unstable in a near neutral to alkaline environment. 
     
     
         69 . The composition of  claim 68 , wherein the delayed-release coating comprise polymethacrylate. 
     
     
         70 . The composition of  claim 69 , wherein the polymethacrylate is a 1:1 copolymer of polymethacrylic acid and ethyl acrylate. 
     
     
         71 . The composition of  claim 60 , further comprising a sealing coat disposed over the coats comprising Larazotide acetate. 
     
     
         72 . The composition of  claim 71 , wherein the sealing coat comprises sugar, polyethylene glycol, polyvinylpyrrolidone, polyvinyl alcohol, polyvinyl acetate, hydroxypropyl cellulose, methylcellulose, ethylcellulose, and/or hydroxypropylmethylcellulose (HPMC). 
     
     
         73 . The composition of  claim 60 , further comprising a top coat outside of the delayed-release particles. 
     
     
         74 . The composition of  claim 73 , wherein the top coat comprises sugar, polyethylene glycol, polyvinylpyrrolidone, polyvinyl alcohol, polyvinyl acetate, hydroxypropyl cellulose, methylcellulose, ethylcellulose, and/or hydroxypropylmethylcellulose (HPMC). 
     
     
         75 . The composition of  claim 60 , wherein the base coat comprising Larazotide acetate further comprise a pharmaceutically-acceptable binder. 
     
     
         76 . The composition of  claim 75 , wherein the binder comprises a natural sugar, starch, gelatin, corn sweetener, gum, carboxymethylcellulose, polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose, ethylcellulose, polymethacrylate, polyethylene glycol, or wax. 
     
     
         77 . The composition of  claim 60 , further comprising an inert processing aid and/or plasticizer. 
     
     
         78 . The composition of  claim 77 , wherein the inert processing aid comprises silicon dioxide, talc, and/or magnesium stearate. 
     
     
         79 . The composition of  claim 77 , wherein the plasticizer comprises citric acid ester, triacetin, phthalic acid ester, dibutyl sebacate, cetyl alcohol, polyethylene glycol, and/or polysorbate.