Fast disintegrating tablet

Abstract

An oral disintegrating tablet that forms liquid crystalline particles or liquid crystalline bulk phase upon disintegration. The oral disintegrating tablet is fast disintegrating following contact with saliva and/or the oral mucosa but also provides slowed delivery of the active ingredient to avoid the difficulties associated with the speed of delivery of an active ingredient through the oral mucosa.

1 . An oral disintegrating tablet suitable for systemic administration of an active ingredient to via the oral mucosa comprising
 an amphiphilic compound capable of self-assembling into liquid crystalline particles when contacted by a hydrophilic solvent;   a therapeutically effective amount of an active ingredient; and   a pharmaceutically acceptable disintegrant;   
       wherein the tablet disintegrates in less than 2 minutes. 
     
     
         2 . (canceled) 
     
     
         3 . The tablet according to  claim 1 , wherein the tablet is capable of adhering to the oral mucosa. 
     
     
         4 . The tablet according to  claim 1 , wherein when the tablet contacts a hydrophilic solvent the amphiphilic compound self-assembles into liquid crystalline particles. 
     
     
         5 . The tablet according to  claim 1 , wherein the tablet prolongs the release of the active ingredient. 
     
     
         6 . The tablet according to  claim 5 , wherein the release of the active ingredient is prolonged compared to release of the same active ingredient from an immediate release oral tablet. 
     
     
         7 . The tablet according to  claim 1 , wherein the oral disintegrating tablet disintegrates in 1 to 60 seconds. 
     
     
         8 . The tablet according to  claim 1 , wherein the amphiphilic compound has one or more of the groups selected from a critical packing parameter (CPP) of >½ and a hydrophilic lipophilic balance (HLB) of 0 to <10. 
     
     
         9 . The tablet according to  claim 1 , wherein the amphiphilic compound has the structure of Formula (I):
   X-T  Formula (I)
   wherein   
       X is selected from the group consisting of an ester, ether, anhydride, amide, amine, carbamide, glycerol, biuret, phenyl, pyridine or phosphate having at least 2 hydrogen bond forming functional groups; and 
       T is selected form the group consisting of:
 (i) a single C 12  to C 18  alkyl, alkenyl and alkynyl terminally attached to X optionally comprising:
 a. one or more double bonds (preferably cis and at about C7 to C11); or 
 b. three or more methyl branches (preferably isoprenoid branching); 
 
 
       and
 (ii) two C 12  to C 18  alkyl, alkenyl and alkynyl both terminally attached to X. 
 
     
     
         10 . The tablet according to  claim 1 , wherein the active ingredient has a log P of −0.5 to 6.4 and/or a molecular weight of 100 to 1200. 
     
     
         11 . The tablet according to  claim 1 , wherein the oral disintegrating tablet retains about 90% or more of the active ingredient following storage at 25° C./60% RH for at least 6 months. 
     
     
         12 . The tablet according to  claim 1 , wherein the disintegrant is about 10 to about 50% w/w of the tablet. 
     
     
         13 . (canceled) 
     
     
         14 . The tablet according to  claim 1 , wherein the disintegrant is sodium starch glycolate, crosslinked polyvinylpyrrolidone or both. 
     
     
         15 . The tablet according to  claim 4 , wherein the liquid crystalline particles form lamella phase, cubic phase or hexagonal phase. 
     
     
         16 . The tablet according to  claim 1 , wherein the amphiphilic compound is a glycerol monoleate. 
     
     
         17 . The tablet according to  claim 1 , wherein the amphiphilic compound is 1 to 20% w/w of the tablet. 
     
     
         18 . The tablet according to  claim 1 , wherein the active ingredient is 0.5 to 10% w/w of the tablet. 
     
     
         19 . (canceled) 
     
     
         20 . A method of administering an active ingredient via the oral mucosa comprising administration of the tablet according to  claim 1 . 
     
     
         21 . The method of  claim 20 , wherein the maximum blood concentration of the active ingredient occurs over 30 minutes following administration of the tablet. 
     
     
         22 . The tablet according to  claim 1 , wherein the oral disintegrating tablet disintegrates in 1 to 10 seconds. 
     
     
         23 . The tablet according to  claim 1 , wherein the oral disintegrating tablet is for sublingual or buccal administration.