Modular systems for the controlled release of a substance with space and time control

Abstract

The present invention concerns an innovative pharmaceutical form for controlled drug release. In particular, the present invention refers to systems obtained by the assembly of individual release modules, of which the capacity to release the drug in time and in space depends on the way in which the modules have been assembled. The modular structure offers high reproducibility of manufacture and flexibility of release.

1 - 13  (canceled).  
     
     
         14 . Module for controlled drug release in the gastrointestinal tract, composed of a matrix of biocompatible polymers comprising optionally an active principle and excipients generally recognised as safe, said module being of cylindrical or polyhedric shape characterised in that it has 
 in the case of cylindrical shape, at least one concave cylinder base;    in the case of polyhedric shape, at least one concave face of the polyhedron.    
     
     
         15 . Module according to  claim 14 , said module being of cylindrical or polyhedric shape characterised in that it has 
 in the case of cylindrical shape, one base of the cylinder concave and the other convex;    in the case of polyhedric shape, at least one of the faces of the polyhedron concave and at least one other of the faces of the polyhedron convex.    
     
     
         16 . Module according to  claim 14 , characterised in that the biocompatible polymer is a hydrophilic polymer and in particular is chosen from the group consisting of polyvinylpyrrolidone, hydroxypropylmethylcellulose, carboxymethylcellulose, hydroxypropyl-cellulose, hydroxyethylcellulose, carboxypolymethylene, guar gum, xanthan gum, chitosanes, gum arabic, carrageenan, sodium and calcium alginates, gelatine and pectins.  
     
     
         17 . Module according to  claim 15 , characterised in that the biocompatible polymer is a hydrophilic polymer and in particular is chosen from the group consisting of polyvinylpyrrolidone, hydroxypropylmethylcellulose, carboxymethylcellulose, hydroxypropyl-cellulose, hydroxyethylcellulose, carboxypolymethylene, guar gum, xanthan gum, chitosanes, gum arabic, carrageenan, sodium and calcium alginates, gelatine and pectins.  
     
     
         18 . Module according to  claim 16 , characterised in that the matrix also comprises a hydrophobic substance chosen from hydrogenated oils, cetyl, myristic and stearyl alcohol, and esters of fatty acids.  
     
     
         19 . Module according to  claim 17 , characterised in that the matrix also comprises a hydrophobic substance chosen from hydrogenated oils, cetyl, myristic and stearyl alcohol, and esters of fatty acids.  
     
     
         20 . Module according to  claim 18 , characterised in that the matrix also comprises an effervescent substance, preferably a mixture of salts that release CO2 in contact with gastrointestinal liquids.  
     
     
         21 . Module according to  claim 19 , characterised in that the matrix also comprises an effervescent substance, preferably a mixture of salts that release CO2 in contact with gastrointestinal liquids.  
     
     
         22 . Module according to  claim 14 , characterised in that it has dimensions suitable for administration by mouth.  
     
     
         23 . Assembly of at least two modules according to  claim 14 .  
     
     
         24 . Assembly according to  claim 23  obtained by fitting together the convex bases/faces and the concave bases/faces of the respective modules and possible subsequent gluing or welding, in particular thermal welding or ultrasound welding.  
     
     
         25 . Assembly according to  claim 24  obtained by placing concave bases/faces of different modules adjacent to each other or by placing concave bases/faces of first modules adjacent to flat bases/faces of second modules, in such a way as to create at least one hollow space in the aggregate and subsequent gluing or welding together of the respective bases or faces.  
     
     
         26 . Assembly of at least one module according to  claim 14  with at least one cylindrical element with flat bases or with at least one polyhedric element with flat faces, said assembly being obtained by placing one concave base/face of the module adjacent to a flat base/face of the element, in such a way as to create at least one hollow space in the assembly and subsequent gluing or welding together of the respective bases or faces.  
     
     
         27 . Assembly of at least one module according to  claim 15  with at least one cylindrical element with flat bases or with at least one polyhedric element with flat faces, said assembly being obtained by placing one concave base/face of the module adjacent to a flat base/face of the element, in such a way as to create at least one hollow space in the assembly and subsequent gluing or welding together of the respective bases or faces.  
     
     
         28 . Assembly according to  claim 26  in which at least one of the cavities is filled with an active principle and possible excipients.  
     
     
         29 . Assembly according to  claim 27  in which at least one of the cavities is filled with an active principle and possible excipients.  
     
     
         30 . Capsule of rigid or soft gelatine, containing at least one module according to  claim 14 .  
     
     
         31 . Capsule of rigid or soft gelatine, containing at least one assembly according to  claim 23 .  
     
     
         32 . Capsule of rigid or soft gelatine, containing at least one assembly according to  claim 26 .  
     
     
         33 . Method for the production of a module according to  claim 14  comprising the following steps: 
 the provision of a biocompatible polymer in a granule size suitable for compacting by pressure, and, optionally,    the provision of an active principle and of optional excipients generally recognised as safe,    the mixing of the components provided,    the compression of the mixture of components or of only the granules of biocompatible polymer in a tablet press provided with at least one convex punch for giving a concave base/face to the compressed module thus obtained.    
     
     
         34 . Method for the production of an assembly according to  claim 23  comprising fitting together the convex bases/faces and the concave bases/faces of the respective modules and subsequent gluing or welding, in particular thermal welding or ultrasound welding.  
     
     
         35 . Method for the production of an assembly according to  claim 26  comprising fitting together a flat base/face of an element and the concave base/face of a module and subsequent gluing or welding, in particular thermal welding or ultrasound welding.