Sublingual buccal effervescent

Abstract

A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administrable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.

1 . A method of manufacturing a tablet suitable for direct oral administration across the oral mucosa, said method comprising the steps of: 
 a) selecting a pharmaceutically effective amount of an orally administrable medicament;    b) selecting at least one saliva activated effervescent couple and determining what amount of same will be necessary to provide for both tablet disintegration and an increase in either the rate or extent of absorption of said orally administrable medicament across the oral mucosa, wherein said amount of said at least one effervescent couple ranges from about 5% by weight to about 80% by weight;    c) producing a mixture from said medicament and said saliva activated effervescent couple; and    d) compressing at least a portion of said mixture so as to form at least one tablet.    
     
     
         2 . The method of  claim 1 , further comprising the step of selecting a bioadhesive and producing said mixture including same.  
     
     
         3 . The method of  claim 1 , further comprising the step of: selecting a non-effervescent disintegration agent and producing said mixture including same.  
     
     
         4 . The method of  claim 1 , further comprising the step of: selecting one or more glidants, lubricants, binders, sweeteners, flavoring and coloring components and producing said mixture including same.  
     
     
         5 . The method of  claim 1 , wherein said orally administrable medicament is selected from the group consisting of analgesics, anti-inflammatories, antipyretics, antibiotics, antimicrobials, laxatives, anorexics, antihistamines, antiasthmatics, antidiuretics, antiflatulents, anti-emetics, antimigraine agents, antispasmodics, sedatives, antihyperactives, antihypertensives, tranquilizers, decongestants, and beta blockers.  
     
     
         6 . The method of  claim 1 , wherein said orally administrable medicament is selected from the group consisting of peptides, proteins and oligonucleotides.  
     
     
         7 . The method of  claim 1 , wherein said at least one saliva activated effervescent agent is present in an amount between about 20% by weight and 80% by weight.  
     
     
         8 . A method of manufacturing a tablet suitable for direct oral administration across the oral mucosa, said method comprising the steps of: 
 a) selecting at least one orally administrable medicament capable of existing in an ionized form and a unionized form in aqueous environment and determining a pharmaceutically effective amount of same;    b) selecting at least one saliva activated effervescent couple and determining what amount of same will be necessary to provide for both tablet disintegration and an increase in either the rate or extent of absorption of said orally administrable medicament across the oral mucosa;    c) selecting a pH adjusting substance and determining what amount of same is sufficient to change the pH of a local environment of said tablet at a site of absorption in the mouth to favor said unionized form of said medicament;    d) producing a mixture from said medicament, said selected saliva activated effervescent couple and said pH adjusting substance, in said predetermined amounts; and    e) compressing at least a portion of said mixture so as to form at least one tablet.    
     
     
         9 . The method of  claim 8 , further comprising the step of: selecting one or more glidants, lubricants, binders, sweeteners, flavoring and coloring components and producing said mixture including same.  
     
     
         10 . The method of  claim 8 , wherein said orally administrable medicament is selected from the group consisting of analgesics, anti-inflammatories, antipyretics, antibiotics, antimicrobials, laxatives, anorexics, antihistamines, antiasthmatics, antidiuretics, antiflatulents, anti-emetics, antimigraine agents, antispasmodics, sedatives, antihyperactives, antihypertensives, tranquilizers, decongestants, and beta blockers.  
     
     
         11 . The method of  claim 8 , wherein said orally administrable medicament is selected from the group consisting of peptides, proteins and oligonucleotides.  
     
     
         12 . The method according to  claim 8 , wherein said at least one effervescent agent is present in an amount between about 5% by weight and 95% by weight.  
     
     
         13 . The method according to  claim 8 , wherein said at least one effervescent agent is present in an amount between about 5% by weight and 80% by weight.  
     
     
         14 . The method according to  claim 13 , wherein said at least one effervescent agent is present in an amount between about 20% by weight and 80% by weight.  
     
     
         15 . The method according to  claim 8 , wherein said at least one effervescent agent is present in an amount sufficient to evolve a gas in an amount between about 5 cm 3  to about 30 cm 3 .  
     
     
         16 . The method according to  claim 8 , wherein said pH adjusting substance is a base.  
     
     
         17 . The method according to  claim 16 , wherein said base is selected from the group consisting of sodium carbonate, potassium carbonate, magnesium carbonate, disodium hydrogen phosphate, sodium dihydrogen phosphate, dipotassium hydrogen phosphate, and potassium dihydrogen phosphate.  
     
     
         18 . The method according to  claim 8 , wherein said pH adjusting substance is an acid.