Oral Composition

Abstract

The present invention relates to a tablet composition comprising a particle and a pharmaceutically acceptable carrier, wherein the particle comprises an amorphous structure and a submicron domain, and wherein the amorphous structure is a molecular solid dispersion of a drug in a polymeric matrix and the submicron domain is a submicron drug particle. The tablet may further comprise a micronized drug particle. The pharmaceutically acceptable carrier comprises a binder, a filler, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent.

We claim: 
     
         1 . An oral tablet composition comprising: (1) a drug particle essentially consisting of an amorphous structure and a submicron domain and (2) a carrier, wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4, and wherein the average diameter of the oral particle is from mesh 20 to mesh 100. 
     
     
         2 . The oral tablet composition as claimed in  claim 1 , wherein the amorphous structure comprises a drug and an amphiphilic polymer, wherein the submicron domain essentially consists of a drug. 
     
     
         3 . The oral tablet composition as claimed in  claim 2 , wherein the amphiphilic polymer is polyvinylpyrrolidone. 
     
     
         4 . The oral tablet composition as claimed in  claim 3 , wherein more than 100 parts water is needed to dissolve 1 part drug. 
     
     
         5 . The oral tablet composition as claimed in  claim 3 , wherein more than 1000 parts water is needed to dissolve 1 part drug. 
     
     
         6 . The oral tablet composition as claimed in  claim 3 , wherein more than 10,000 parts water is needed to dissolve 1 part drug. 
     
     
         7 . An oral tablet composition comprising: (1) a drug particle essentially consisting of an amorphous structure and a submicron domain and (2) a carrier, wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4, wherein the average diameter of the oral particle is from mesh 20 to mesh 100, wherein more than 100 parts water is needed to dissolve 1 part drug; wherein the amorphous structure comprises a drug and polyvinylpyrrolidone, and wherein the submicron domain essentially consists of a drug. 
     
     
         8 . The oral tablet composition as claimed in  claim 7 , wherein the oral tablet composition comprises a micronized drug particle. 
     
     
         9 . The oral tablet composition as claimed in  claim 7 , wherein the amount of the drug in the oral tablet composition is more than 30%. 
     
     
         10 . The oral tablet composition as claimed in  claim 7 , wherein the amount of the drug in the oral tablet composition is more than 50%. 
     
     
         11 . The oral tablet composition as claimed in  claim 7 , wherein the amount of the drug in the oral tablet composition is more than 70%. 
     
     
         12 . The oral tablet composition as claimed in  claim 7 , the carrier comprises a binder, a filler, a disintegrant, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent. 
     
     
         13 . The oral tablet composition as claimed in  claim 12 , the carrier optionally comprises an acid-soluble polymer and the oral tablet composition is optionally coated with an enteric film. 
     
     
         14 . The oral tablet composition as claimed in  claim 13 , the acid-soluble polymer is a cationic copolymer based on dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate. 
     
     
         15 . The oral tablet composition as claimed in  claim 10 , the carrier comprises a binder, a filler, a disintegrant, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent. 
     
     
         16 . The oral tablet composition as claimed in  claim 15 , the disintegrant is selected from the group consisting of crospovidone; carboxyalkyl celluloses, low substituted hydroxypropyl cellulose, crosslinked carboxyalkylcellulose and their alkali salts; pregelatinized starch, dried starch, sodium starch glycolate; resins; and mixtures thereof. 
     
     
         17 . The oral tablet composition as claimed in  claim 15  the carrier optionally comprises an acid-soluble polymer and the oral tablet composition is optionally coated with an enteric film. 
     
     
         18 . The oral tablet composition as claimed in  claim 15 , the carrier optionally comprises a gas-producing ingredient. 
     
     
         19 . The oral tablet composition as claimed in  claim 18 , the gas-producing ingredient is selected from the group consisting of calcium carbonate, sodium bicarbonate, potassium bicarbonate, sodium sulfite, sodium bisulfite, sodium metabisulfite, citric acid, malic acid, succinic acid, tartaric acid, fumaric acid, maleic acid, ascorbic acid, glutamic acid, their salts, and mixtures thereof. 
     
     
         20 . An oral tablet composition comprising: (1) a drug particle comprising an amorphous structure and a submicron domain and (2) a carrier, wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4, wherein the average diameter of the oral particle is from mesh 20 to mesh 100, wherein the oral tablet composition optionally comprises a micronized drug particle, and wherein the drug is ezetimibe.