Directly compressible composition comprising microcrystalline cellulose

Abstract

The present invention relates to a directly compressible composition for the production of tablets which comprise fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs) in a co-mixture. The present invention also relates to the use of this mixture and to a process for the preparation thereof.

1 . Directly compressible co-mixtures comprising fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs). 
     
     
         2 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained microcrystalline celluloses having average particle sizes of D v50 <100 μm, preferably having average particle sizes of D v50 <70 μm, particularly preferably having average particle sizes in the D v50  range 17 to 67 μm, in particular in the D v50  range 17 μm-20 μm. 
     
     
         3 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained polyvinyl alcohols to fine-grained microcrystalline celluloses in a ratio of 5:1 to 1:5, preferably 2:1 to 1:2, especially preferably in a ratio of 1:1, based on the weight. 
     
     
         4 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained polyvinyl alcohols which meet the requirements of the pharmacopoeias (Ph. Eur., USP and JPE) and which are suitable for retardation of active compound. 
     
     
         5 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained polyvinyl alcohols of grades 4-88, 18-88, 26-88 and 40-88, which meet the requirements of the pharmacopoeias Ph, Eur, JPE and USP, and grade 28-99, which conforms to the pharmacopoeias JPE and Ph. Eur. 
     
     
         6 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained polyvinyl alcohols (PVAs) which conform to Ph. Eur. and which have been obtained by polymerisation of vinyl acetate and by subsequent partial of virtually complete hydrolysis of the polyvinyl acetate and have an average relative molecular weight in the range between 20,000 and 150,000 g/mol, and which have a viscosity, in accordance with Ph. Eur., in the range 3-70 mPa·s, (measured in a 4% solution at 20° C.) and have an ester value of not greater than 280 mg of KOH/g (degree of hydrolysis >72.2 mol %). 
     
     
         7 . Directly compressible co-mixtures according to  claim 1 , comprising fine-grained polyvinyl alcohols (PVAs) which conform to the USP and are in the form of water-soluble, synthetic resins which are characterised by the formula
   (C 2 H 4 O) n      in which   n denotes an integer in the range of 500 to 5000, and which have been obtained by 85-89% hydrolysis of the polyvinyl acetate.   
     
     
         8 . Active compound-containing tablets having extended release of active compound, comprising fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs). 
     
     
         9 . Active compound-containing tablets having extended release of active compound of several hours, comprising a co-mixture of fine-grained polyvinyl alcohols (PVAs) and fine-grained microcrystalline celluloses (MCCs) according to  claim 1 . 
     
     
         10 . Active compound-containing tablets according to  claim 8 , comprising a directly compressible co-mixture comprising PVAs and MCCs in an amount in the range 1-99% by weight, preferably in an amount of 5-95% by weight, very particularly preferably in an amount of 10-90% by weight, based on the total weight of the tablet. 
     
     
         11 . Active compound-containing tablets according to  claim 8 , which, in the case of production using low pressing forces, give tablets having particularly high tablet hardnesses and low friabilities of ≦0.2% by weight, but where only low ejection forces have to be used. 
     
     
         12 . Active compound-containing tablets according to  claim 8  having delayed release of active compound, comprising active compounds in BCS class I, either alone or in combination with other active compounds. 
     
     
         13 . A method for the production of tablets, where tablets having hardnesses of ≧153 N with a friability of ≦0.2% by weight are obtained by compression with a pressing force of 10 kN, comprising preparing said tablets from directly compressible co-mixtures according to  claim 1 . 
     
     
         14 . A method for the production of tablets, where tablets having hardnesses of ≧289 N with a friability of <0.1% by weight are obtained by compression with a pressing force of 20 kN, comprising preparing said tablets from directly compressible co-mixtures according to  claim 1 .