Use Of Polyether-Based And Vinyl Monomer-Based Copolymers As Binders For Dosing Forms Comprising Solid Active Ingredients

Abstract

The use of water-soluble or water-dispersible copolymers which are obtained by free radical-initiated polymerization of a mixture of i) 30 to 80% by weight N-vinyllactam, ii) 10 to 50% by weight vinylacetate and iii) 10 to 50% by weight of a polyether, with the proviso that the total of i), ii) and iii) is equal to 100% by weight, as binders for producing solid active ingredient-containing dosage forms.

1 . A solid active ingredient-containing dosage form comprising binders that include water-soluble or water-dispersible copolymers which are obtained by free radical-initiated polymerization of a mixture of
 i) 30 to 80% by weight of N-vinyllactam,   ii) 10 to 50% by weight of vinyl acetate and   iii) 10 to 50% by weight of a polyether,   
       with the proviso that the total of i), ii) and iii) is equal to 100% by weight. 
     
     
         2 . The solid active ingredient-containing dosage form according to  claim 1 , wherein the copolymers are obtained from
 i) 30 to 70% by weight of N-vinyllactam   ii) 15 to 35% by weight of vinyl acetate, and   iii) 10 to 35% by weight of a polyether,   
       is employed. 
     
     
         3 . The solid active ingredient-containing dosage form according to  claim 2 , wherein the copolymers are obtained from
 i) 40 to 60% by weight of N-vinyllactam   ii) 15 to 35% by weight of vinyl acetate   iii) 10 to 30% by weight of a polyether.   
     
     
         4 . The solid active ingredient-containing dosage form according to  claim 1 , in the form of a tablets. 
     
     
         5 . The solid active ingredient-containing dosage form according to  claim 1 , comprising the binders in an amount of from 1 to 20% by weight based on the total weight of the dosage form. 
     
     
         6 . The solid active ingredient-containing dosage form according to  claim 5 , comprising the binders in an amount of from 1 to 10% by weight in the dosage forms. 
     
     
         7 . The solid active ingredient-containing dosage form according to  claim 1 , wherein the binders are employed as dry binders. 
     
     
         8 . The solid active ingredient-containing dosage form according to  claim 7 , wherein the binders are employed as dry binders for direct tableting. 
     
     
         9 . The solid active ingredient-containing dosage form according to  claim 1 , wherein the binders are employed in the form of wet granules or fluidized-bed granules. 
     
     
         10 . The solid active ingredient-containing dosage form according to  claim 1 , wherein the binders are in the form of sintered granules. 
     
     
         11 . The solid active ingredient-containing dosage form according to  claim 10 , where the sintered granules are obtained at temperatures of 50 to 100° C. 
     
     
         12 . The solid active ingredient-containing dosage form according to  claim 11 , where the sintered granules are obtained at temperatures of 70 to 100° C. 
     
     
         13 . The solid active ingredient-containing dosage form according to  claim 1 , where the binders are granulated in the presence of further pharmaceutical excipients. 
     
     
         14 . The solid active ingredient-containing dosage form according to  claim 1 , where the binders are granulated in the presence of active pharmaceutical ingredients. 
     
     
         15 . A process for producing a solid pharmaceutical dosage form, which comprises mixing, as binders, water-soluble or water-dispersible copolymers which are obtained by free radical-initiated polymerization of a mixture of
 i) 30 to 80% by weight of N-vinyllactam,   ii) 10 to 50% by weight of vinyl acetate and   iii) 10 to 50% by weight of a polyether,   
       with the proviso that the sum of i), ii) and iii) is equal to 100% by weight, with active pharmaceutical ingredients and optionally further pharmaceutical excipients, and subsequently converting the mixture into the solid pharmaceutical dosage form. 
     
     
         16 . The process according to  claim 15 , wherein the binders are mixed dry with the active pharmaceutical ingredients and optionally the further pharmaceutical excipients to form a dry mixture, and the dry mixture is converted into the solid pharmaceutical dosage forms. 
     
     
         17 . The process according to  claim 16 , wherein the binders are incorporated in the form of granules into the solid pharmaceutical dosage form. 
     
     
         18 . The process according to  claim 17 , wherein the granules are obtained by wet granulation, fluidized-bed granulation or sinter granulation. 
     
     
         19 . The process according to  claim 17 , wherein further pharmaceutical excipients are incorporated into the granules. 
     
     
         20 . The process according to  claim 17 , wherein the active pharmaceutical ingredients are incorporated into the granules. 
     
     
         21 . The process according to  claim 15 , wherein the mixture of the binders, the active pharmaceutical ingredients and the optionally further pharmaceutical excipients is converted by compression into the solid dosage form.