Tamper-resistant tablet providing immediate drug release

Abstract

The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material; and method of using said tablet to treat pain and other conditions.

1 . A tamper-resistant tablet comprising:
 (i) a matrix material in an amount of more than one third of the total weight of the tablet; and   (ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet;   wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide;   wherein said pharmacologically active compound is selected from the group consisting of stimulants; and   wherein said particulates form a discontinuous phase within the matrix material.   
     
     
         2 . The tablet according to  claim 1 , wherein the pharmacologically active compound is selected from the group consisting of amphetamine, amphetaminil, lisdexamphetamine dimesylate, metamphetamine, methylphenidate, and physiologically acceptable salts thereof. 
     
     
         3 . The tablet according to  claim 2 , wherein the pharmacologically active compound is amphetamine or a physiologically acceptable salt thereof. 
     
     
         4 . The tablet according to  claim 2 , wherein the pharmacologically active compound is methylphenidate or a physiologically acceptable salt thereof. 
     
     
         5 . The tablet according to  claim 1 , which provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur. 
     
     
         6 . The tablet according to  claim 5 , which has under in vitro conditions a disintegration time measured in accordance with Ph. Eur. of at most 3 minutes. 
     
     
         7 . The tablet according to  claim 1 , wherein the content of the matrix material is at least 40 wt.-%, based on the total weight of the tablet. 
     
     
         8 . The tablet according to  claim 1 , wherein the particulates have an average diameter of about 1000±250 μm and/or an average length of about 750±250 μm. 
     
     
         9 . The tablet according to  claim 1 , wherein the pharmacologically active compound is dispersed in the polyalkylene oxide. 
     
     
         10 . The tablet according to  claim 1 , wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of a particulate. 
     
     
         11 . The tablet according to  claim 1 , wherein the content of the pharmacologically active compound is at least 25 wt.-%, based on the total weight of a particulate. 
     
     
         12 . The tablet according to  claim 1 , wherein the particulates are hot melt-extruded. 
     
     
         13 . The tablet according to  claim 1 , wherein the particulates are film coated. 
     
     
         14 . The tablet according to  claim 1 , wherein the matrix material is also present in particulate form. 
     
     
         15 . The tablet according to  claim 1 , wherein the matrix material is dry granulated or compacted. 
     
     
         16 . The tablet according to  claim 1 , wherein the matrix material comprises binder, filler, disintegrant and/or lubricant. 
     
     
         17 . The tablet according to  claim 16 , wherein the disintegrant is crosslinked. 
     
     
         18 . A method of treating a condition treatable with a stimulant in a patient in need thereof by administering to said patient a tablet comprising an effective amount therefor of a pharmacologically active compound, wherein the tablet is a tablet according to  claim 1 .