5-aminosalicylic acid capsule formulation

Abstract

A dosage form comprising a capsule containing one or more tablets of 5-aminosalicylic acid or a salt thereof as an active ingredient where each of the one or more tablets is enterically coated is disclosed.

1 .- 3 . (canceled) 
     
     
         4 . A dosage form comprising:
 (a) a capsule shell; and   (b) at least one tablet within the capsule shell, the at least one tablet containing 5-aminosalicylic acid or a salt thereof as an active ingredient and having an enteric coat that prevents release of the 5-aminosalicylic acid in the upper gastrointestinal tract, wherein the capsule shell has less than about 10% by weight moisture content at a relative humidity of 60% and a temperature of 25° C.   
     
     
         5 . The dosage form according to  claim 4 , wherein the dosage form is stable. 
     
     
         6 . The dosage form according to  claim 5 , wherein no more than 0.15% w/w 5-[2-formyl-5-(hydroxymethyl-1H-pyrrol-1-yl]-2-hydroxybenzoic acid accumulates upon storage of the dosage form at a relative humidity of 60% and a temperature of 25° C. for a period of at least six months. 
     
     
         7 . The dosage form according to  claim 4 , wherein the capsule shell comprises gelatin, hydroxypropylmethyl cellulose, polyvinyl alcohol, or a combination thereof. 
     
     
         8 . The dosage form according to  claim 4 , wherein the capsule shell comprises hydroxypropylmethyl cellulose. 
     
     
         9 . The dosage form according to  claim 4 , wherein the at least one tablet comprises a reducing sugar. 
     
     
         10 . The dosage form according to  claim 4 , wherein the capsule shell contains one, two, three, four or five tablets. 
     
     
         11 . The dosage form according to  claim 4 , wherein the at least one tablet contains from about 50 mg to about 1,800 mg of 5-aminosalicylic acid. 
     
     
         12 . The dosage form according to  claim 4 , wherein the enteric coat comprises a material capable of delivering the 5-aminosalicylic acid to the colon of a human. 
     
     
         13 . The dosage form according to  claim 4 , wherein the enteric coat comprises a material selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof. 
     
     
         14 . The dosage form according to  claim 4 , wherein the enteric coat further comprises a plasticizer. 
     
     
         15 . The dosage form according to  claim 14 , wherein the plasticizer is selected from the group consisting of polyethylene glycols, propylene glycols, 1,2-propylene glycol, dibutyl phthalate, dibutyl sebacate, diethyl phthalate, tributyl citrate, triethyl citrate, tributyrin, butyl phthalyl butyl glycolate, triacetin, castor oil, citric acid esters, and combinations thereof. 
     
     
         16 . The dosage form according to  claim 4 , wherein the enteric coat further comprises inert solid particulates. 
     
     
         17 . The dosage form according to  claim 16 , wherein the inert solid particulates comprise a material selected from the group consisting of talc, iron oxide, titanium dioxide, and combinations thereof. 
     
     
         18 . The dosage form according to  claim 4 , wherein the enteric coat comprises a single enteric coating. 
     
     
         19 . The dosage form according to  claim 4 , wherein the enteric coat comprises a plurality of enteric coatings. 
     
     
         20 . The dosage form according to  claim 4 , wherein the total thickness of the enteric coat ranges from about 50 μm to about 250 μm. 
     
     
         21 . The dosage form according to  claim 4 , wherein the enteric coat comprises an inner layer of a first polyacrylic acid copolymer enteric coating and an outer layer of a polyacrylic acid copolymer enteric coating that is different than the inner layer. 
     
     
         22 . The dosage form according to  claim 21 , wherein the inner layer of enteric coating is poly(methacrylic acid, methyl methacrylate) 1:2 and the outer layer of enteric coating is poly(methacrylic acid, methyl methacrylate) 1:1. 
     
     
         23 . The dosage form according to  claim 4 , wherein the capsule does not have an enteric coating. 
     
     
         24 . The dosage form according to  claim 4 , wherein a drug-release profile of the dosage form is pH dependent. 
     
     
         25 . The dosage form according to  claim 4 , wherein the at least one tablet is greater than 5 mm in diameter. 
     
     
         26 . A kit comprising:
 a dosage form according to  claim 4 ; and   a predetermined amount of desiccant.   
     
     
         27 . A method of treating an inflammatory condition of the lower gastrointestinal tract comprising administering a dosage form according to  claim 4  to a patient in need of treatment. 
     
     
         28 .- 30 . (canceled) 
     
     
         31 . The dosage form according to  claim 10 , wherein the capsule shell contains one tablet. 
     
     
         32 . The dosage form according to  claim 8 , wherein the at least one tablet comprises a reducing sugar. 
     
     
         33 . The dosage form according to  claim 32 , wherein the at least one tablet is greater than 5mm in diameter. 
     
     
         34 . The dosage form according to  claim 33 , wherein the capsule shell contains one tablet. 
     
     
         35 . A dosage form comprising:
 (a) a capsule shell; and   (b) at least one tablet within the capsule shell, the at least one tablet containing 5-aminosalicylic acid or a salt thereof as an active ingredient and having an enteric coat that prevents release of the 5-aminosalicylic acid in the upper gastrointestinal tract,   wherein the capsule shell has a moisture content such that no more than 0.15% w/w 5-[2-formyl-5-(hydroxymethyl-1H-pyrrol-1-yl]-2-hydroxybenzoic acid accumulates upon storage of the dosage form at a relative humidity of 60% and a temperature of 25° C. for a period of at least six months.