Controlled Release Dosage Forms

Abstract

The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

1 . A stable controlled release monolithic coating composition for use in coating a pharmaceutical oral dosage form, said coating comprising:
 a) an aqueous dispersion of a neutral ester copolymer without any functional groups;   b) a poly glycol having a melting point greater than 55° C., and   c) one or more pharmaceutically acceptable excipients;   
       wherein said coating composition is coated onto said pharmaceutical oral dosage form and cured at a temperature at least equal to or greater than the melting point of said poly glycol. 
     
     
         2 . The stable controlled release coating composition of  claim 1  wherein said neutral ester copolymer without any functional groups is selected from the group consisting of Eudragit NE30D, Eudragit NE40D and any combination thereof. 
     
     
         3 . The stable controlled release coating composition of  claim 2  wherein said neutral ester copolymer without any functional groups is NE30D. 
     
     
         4 . The stable controlled release coating composition of claim of  claim 1  wherein said neutral ester copolymer without any functional groups is present in an amount of from about 1% to about 35% by weight of the coating composition. 
     
     
         5 . The stable controlled release coating composition of  claim 4  wherein said neutral ester copolymer without any functional groups is present in an amount of from about 1% to about 25% by weight of the coating composition. 
     
     
         6 . The stable controlled release coating composition of  claim 5  wherein said neutral ester copolymer without any functional groups is present in an amount of from about 1% to about 7%. 
     
     
         7 . The stable controlled release coating composition of  claim 1  wherein said poly glycol is selected from the group consisting of polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 20000, Poloxamer 188, Poloxamer 338, Poloxamer 407, Polyethylene Oxides, Polyoxyethylene Alkyl Ethers, Polyoxyethylene Sorbitan Fatty Acid Esters, and Polyoxyethylene Stearates. 
     
     
         8 . The stable controlled release coating composition of  claim 1  wherein said poly glycol is selected from the group consisting of polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 20000 and any combination thereof. 
     
     
         9 . (canceled) 
     
     
         10 . The stable controlled release coating composition of  claim 1  wherein said polyethylene glycol or derivative thereof is present in an amount of from about 0.1% to about 10% by weight of the coat composition. 
     
     
         11 - 13 . (canceled) 
     
     
         14 . The stable controlled release coating composition of  claim 1  wherein the one or more pharmaceutically acceptable excipients is selected from the group consisting of anti-tacking agents, emulsifying agents, hydrophilic agents, antifoaming agents, flavourants, colourants, sweeteners and any combination thereof. 
     
     
         15 . The stable controlled release coating composition of  claim 14  wherein the anti-tacking agent is selected from the group consisting of adipic acid, magnesium stearate, calcium stearate, zinc stearate, hydrogenated vegetable oils, sterotex, glyceryl monostearate, talc, sodium benzoate, sodium lauryl sulfate, magnesium lauryl sulfate and any combination thereof. 
     
     
         16 - 18 . (canceled) 
     
     
         19 . The stable controlled release coating composition of  claim 14  wherein said hydrophilic agent is selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose and any combination thereof. 
     
     
         20 - 25 . (canceled) 
     
     
         26 . The stable controlled release coating composition of  claim 14  wherein said anti-foaming agent is present in an amount up to about 0.5% by weight of the coating composition. 
     
     
         27 . (canceled) 
     
     
         28 . The stable controlled release coating composition of  claim 14  wherein said emulsifying agent is selected from the group consisting of polysaccharides, glycerol esters, cellulose ethers, sorbitan esters, polysorbates and any combination thereof. 
     
     
         29 . (canceled) 
     
     
         30 . The stable controlled release coating composition of  claim 28  wherein said polyoxyethylene sorbitan mono-oleate is present in an amount of up to about 0.5% by weight of the coat composition. 
     
     
         31 - 36 . (canceled) 
     
     
         37 . The stable controlled release coating composition of  claim 1  wherein said pharmaceutical oral dosage form is selected from the group consisting of tablets and capsules. 
     
     
         38 . A stable controlled release monolithic coating composition for use in coating a pharmaceutical oral dosage form, said coating comprising an aqueous dispersion of Eudragit NE300, polyethylene glycol 8000, hydroxypropyl methylcellulose, talc, simethicone, titanium dioxide, and polyoxyethylene sorbitan mono-oleate, said Eudragit NE300 is present in an amount of from about 1% to about 35% by weight of the coat composition, said polyethylene glycol is present in an amount of from about 0.1% to about 3% by weight of the coat composition, said hydroxypropyl methylcellulose is present in an amount of from about 0.1% to about 6% by weight of the coat composition, said talc is present in an amount of from about 0.1% to about 7% by weight of the coat composition, said simethicone is present in an amount up to about 0.5% by weight of the coat composition, said polyoxyethylene sorbitan mono-oleate is present in an amount of up to about 0.5% by weight of the coat composition, said titanium dioxide is present in an amount of from about 0% to about 2% by weight of the coat composition; and composition is coated onto said pharmaceutical oral dosage form and cured at a temperature at least equal to or greater than the melting point of said polyglycol. 
     
     
         39 . The controlled release oral dosage form of  claim 38 , wherein said pharmaceutical dosage form is selected from the group consisting of tablets and capsules 
     
     
         40 . A controlled release oral dosage form comprising:
 a) a core, wherein said core comprises:
 i) an effective amount of at least one therapeutically active agent, and 
 ii) one or more first pharmaceutically acceptable excipients, and 
   b) a stable controlled release monolithic coating composition for coating said core, said coating composition comprising:
 i) an aqueous dispersion of a neutral ester copolymer without any functional groups; 
 ii) a poly glycol having a melting point greater than 55° C., and 
 iii) one or more second pharmaceutically acceptable excipients; 
   
       wherein said coating composition is coated onto said core and cured at a temperature at least equal to or greater than the melting point of the poly glycol.