Matrix pellets for greasy, oily or sticky drug substances

Abstract

A drug delivery system for oral administration in solid dry form of greasy/oily/sticky substance(s) and pharmaceutically active substance(s) or pharmaceutically active substance(s) which itself/themselves is/are greasy/oily/sticky) characterized by having a plurality of solid, polymeric matrix beads comprising considerable amounts of greasy/oily/sticky substances and having fast release characteristics and a process for the preparation of such solid, polymeric matrix beads comprising greasy/oily/sticky substances.

1 . A dry, solid drug delivery composition which comprises: 
 (i) at least one greasy, oily or sticky substance and at least one pharmaceutically active substance, or    (ii) at least one greasy, oily or sticky pharmaceutically active substance,    characterized in that the composition is in the form of a plurality of beads containing a polymeric matrix composed of a polyethylene glycol or a mixture of polyethylene glycols being solid at ambient temperature, said composition having fast release characteristics, and containing from 15 wt % to 70 wt % of the component (i) or (ii).    
     
     
         2 . A drug delivery composition according to  claim 1 , wherein the polymeric matrix is composed of a polyethylene glycol having a molecular weight of from 4000 to 20000.  
     
     
         3 . A drug delivery composition according to  claim 1 , wherein the polymeric matrix is composed of a mixture of polyethylene glycols having molecular weights from 4000 to 100000.  
     
     
         4 . A drug delivery composition according to  claim 1 , wherein the polymeric matrix is composed of a mixture of polyethylene glycols having molecular weights from 400 to 100000, provided that they are in such proportions that the resulting matrix beads become solid at ambient temperature.  
     
     
         5 . A drug delivery composition according to any of the preceeding claims wherein the polymeric matrix beads have a particle size of 0.1-10 mm.  
     
     
         6 . A drug delivery composition according to any of the preceeding claims wherein the polymeric matrix beads have a particle size of 0.25-3 mm.  
     
     
         7 . A drug delivery composition according to any of the preceeding claims wherein the content of the greasy, oily and/or sticky substance is in the range from 40% w/w to 70% w/w.  
     
     
         8 . A drug delivery composition according to any of the preceeding claims wherein the pharmaceutically active substance has a molecular weight less than 1000 dalton.  
     
     
         9 . A drug delivery composition according to any of the preceeding claims wherein the pharmaceutically active substance is a thrombin inhibiting peptide drug.  
     
     
         10 . A drug delivery composition according to any of the preceeding claims wherein the pharmaceutically active substance is a dihydropyridine compound.  
     
     
         11 . A drug delivery composition according to  claim 9  wherein the pharmaceutically active substance is melagatran.  
     
     
         12 . A drug delivery composition according to  claim 10  wherein the pharmaceutically active substance is felodipine.  
     
     
         13 . A drug delivery composition according to any of claims  1 - 8  wherein the pharmaceutically active substance is alendronate.  
     
     
         14 . A process for the preparation of a dry, solid drug delivery composition which comprises: 
 (i) at least one greasy, oily or sticky substance and at least one pharmaceutically active substance, or    (ii) at least one greasy, oily or sticky pharmaceutically active substance,    characterized by the transformation from the solid to the liquid state of a polyethylene glycol or a mixture of polyethylene glycols being solid at ambient temperature which will be making up the matrix beads, adding greasy/oily/sticky substance(s) and optionally pharmaceutically active substance(s) and preparing an emulsion/suspension of the obtained mixture, whereafter suitable aliquots/droplets of the obtained polymeric emulsion/suspension are transformed to a plurality of beads in the solid state.    
     
     
         15 . Use of plurality of beads containing a polymeric matrix composed of a polyethylene glycol or a mixture of polyethylene glycols being solid at ambient temperature which beads is contains from 15 wt % to 70 wt % of a component 
 (i) at least one greasy, oily or sticky substance and at least one pharmaceutical active substance, or    (ii) at least one greasy, oily or sticky pharmaceutically active substance,    in the preparation of a dry, solid drug delivery composition having fast release characteristics.