New abuse-resistant pharmaceutical composition for the treatment of opioid dependence

Abstract

There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.

1 - 23 . (canceled) 
     
     
         24 . A method of treatment of opioid dependency and/or addiction, which method comprises administration of a tablet composition suitable for sublingual administration comprising:
 (a) microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof in intimate contact with particles comprising citric acid;   (b) a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof; and   (c) a disintegrant selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone and mixtures thereof.   to a person suffering from, or susceptible to, opioid dependency and/or addiction.   
     
     
         25 . A method as claimed in  claim 24 , wherein the microparticles of buprenorphine or salt thereof have a weight based mean diameter of less than about 15 μm. 
     
     
         26 . A method as claimed in  claim 24  or  claim 25  wherein the tablet composition comprises an interactive mixture comprising microparticles of buprenorphine or salt thereof presented upon the surfaces of carrier particles. 
     
     
         27 . A method as claimed in  claim 26 , wherein the carrier particles are of a size that is between about 100 and about 800 μm. 
     
     
         28 . A method as claimed in  claim 26  or  claim 27 , wherein the carrier particles are water-soluble. 
     
     
         29 . A method as claimed in any one of  claims 26  to  28 , wherein the carrier particles comprise mannitol. 
     
     
         30 . A method as claimed in any one of  claims 26  to  29 , wherein the particles of citric acid are presented and act as carrier particles. 
     
     
         31 . A method as claimed in any one of  claims 24  to  30 , wherein the tablet composition comprises particles comprising naloxone or salt thereof and disintegrant. 
     
     
         32 . A method of treatment of pain, which method comprises administration of a tablet composition suitable for sublingual administration comprising:
 (a) microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof in intimate contact with particles comprising citric acid;   (b) a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof; and   (c) a disintegrant selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone and mixtures thereof.   to a person suffering from or susceptible to, pain.   
     
     
         33 . A method as claimed in  claim 32 , wherein the microparticles of buprenorphine or salt thereof have a weight based mean diameter of less than about 15 μm. 
     
     
         34 . A method as claimed in  claim 32  or  claim 33  wherein the tablet composition comprises an interactive mixture comprising microparticles of buprenorphine or salt thereof presented upon the surfaces of carrier particles. 
     
     
         35 . A method as claimed in  claim 34 , wherein the carrier particles are of a size that is between about 100 and about 800 μm. 
     
     
         36 . A method as claimed in  claim 34  or  claim 35 , wherein the carrier particles are water-soluble. 
     
     
         37 . A method as claimed in any one of  claims 34  to  36 , wherein the carrier particles comprise mannitol. 
     
     
         38 . A method as claimed in any one of  claims 34  to  37 , wherein the particles of citric acid are presented and act as carrier particles. 
     
     
         39 . A method as claimed in any one of  claims 32  to  38 , wherein the tablet composition comprises particles comprising naloxone or salt thereof and disintegrant.