Ion-exchange composition with water-soluble mucoadhesive polymers

1 . An oral tablet for oromucosal delivery of biologically active compounds, the tablet comprising:

i) a sugar alcohol composition in powder form comprising one or more sugar alcohol particles selected from the group consisting of sorbitol particles, erythritol particles, xylitol particles, lactitol particles, maltitol particles, mannitol particles, isomalt particles, and combinations thereof, in an amount of at least 60% by weight of the tablet; and

ii) an ion-exchange composition in powder form, the ion-exchange composition in powder form being located in the tablet as a separate composition mixed with the sugar alcohol composition in powder form, and the ion-exchange composition in powder form comprising a plurality of particles consisting of at least one water-soluble anionic mucoadhesive polymer loaded with nicotine,

wherein an average particle diameter of the plurality of particles consisting essentially of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine is from 10 to 1000 microns,

wherein the at least one water-soluble anionic mucoadhesive polymer is selected from sulfonated polysaccharides, anionic polysaccharides, polyacrylic acid, and combinations thereof,

wherein the plurality of particles consisting of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine are operable to form a gel in contact with the oral mucosa when hydrated with saliva,

wherein the plurality of particles consisting of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine are operable to protect the nicotine until adherence to the oral mucosa,

wherein the weight ratio of the at least one water-soluble anionic mucoadhesive polymer to nicotine is from 2:1 to 20:1, and

wherein the oral tablet is an orally disintegrating tablet.

2 . The oral tablet according to claim 1 , wherein a weight ratio of the at least one water-soluble anionic mucoadhesive polymer to nicotine is from 2:1 to 15:1.

3 . The oral tablet according to claim 1 , wherein the at least one water-soluble anionic mucoadhesive polymer is weakly acidic.

4 . The oral tablet according to claim 1 , wherein the at least one water-soluble anionic mucoadhesive polymer comprises carboxylic functional groups.

5 . The oral tablet according to claim 1 , wherein the at least one water-soluble anionic mucoadhesive polymer is selected from the group consisting of xanthan gum, carrageenan, carbomer, carboxymethyl cellulose and combinations thereof.

6 . The oral tablet according to claim 1 , wherein the oral tablet comprises the ion-exchange composition in an amount of 0.1 to 25% by weight of the tablet.

7 . The oral tablet according to claim 1 , wherein the oral tablet comprises a buffering agent in an amount of 1 to 5% by weight of the tablet.

8 . The oral tablet according to claim 1 , wherein the one or more sugar alcohol particles comprises non-DC sugar alcohol particles selected from non-DC particles of erythritol, maltitol, xylitol, isomalt, and combinations thereof.

9 . The oral tablet according to claim 1 , wherein the one or more sugar alcohol particles comprises at least 20% by weight of non-DC sugar alcohol particles with a particle size above 500 μm.

10 . The oral tablet according to claim 1 , wherein the one or more sugar alcohol particles comprises directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles present in the tablet in a weight ratio between said non-DC sugar alcohol particles and said DC sugar alcohol particles of 0.2 and 1.2.

11 . The oral tablet according to claim 1 , wherein the one or more sugar alcohol particles is tableted into a first module and combined with a second population of particles that is tableted into a second module, and wherein the second module is different in composition than the first module.

12 . The oral tablet according to claim 1 , wherein the one or more sugar alcohol particles is tableted into a first module and combined with a second population of particles that is tableted into a second module, and wherein the second module includes gum base.

13 . The oral tablet according to claim 1 , wherein the oral tablet further comprises a disintegrant in an amount of 1 to 10% by weight of the tablet.

14 . A powder composition comprising:

i) a sugar alcohol composition in powder form comprising one or more sugar alcohol particles selected from the group consisting of sorbitol particles, erythritol particles, xylitol particles, lactitol particles, maltitol particles, mannitol particles, isomalt particles, and combinations thereof, in an amount of at least 60% by weight of the powder composition; and

ii) an ion-exchange composition in powder form for oromucosal delivery of biologically active compounds, the ion-exchange composition comprising:

a plurality of particles consisting of at least one water-soluble anionic mucoadhesive polymer loaded with nicotine,

wherein an average particle diameter of the plurality of particles consisting of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine is from 10 to 1000 microns,

wherein the at least one water-soluble anionic mucoadhesive polymer is selected from the group consisting of xanthan gum, carrageenan, carbomer, carboxymethyl cellulose and combinations thereof,

wherein the plurality of particles consisting of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine are operable to form a gel in contact with the oral mucosa when hydrated with saliva,

wherein the plurality of particles consisting of the at least one water-soluble anionic mucoadhesive polymer loaded with nicotine are operable to protect the biologically active compound until adherence to the oral mucosa, and

wherein the weight ratio of the at least one water-soluble anionic mucoadhesive polymer to nicotine is from 2:1 to 20:1.

15 . The powder composition according to claim 14 , wherein the powder composition is included in a sachet.

16 . The powder composition according to claim 14 , wherein the ion-exchange composition ii) is made by providing a water slurry of the at least one water-soluble anionic mucoadhesive polymer, adding nicotine, and evaporating water from the slurry to obtain a final water content below 10% by weight of the ion exchange composition.

17 . The powder composition according to claim 14 , wherein the ion-exchange composition ii) is made by providing a water dispersion of the at least one water-soluble anionic mucoadhesive polymer, adding nicotine, and precipitating the composition from the dispersion by means of a suitable agent to obtain a final water content below 10% by weight of the ion exchange composition.

18 . A powder composition comprising:

i) a sugar alcohol composition in powder form comprising one or more sugar alcohol particles selected from the group consisting of sorbitol particles, erythritol particles, xylitol particles, lactitol particles, maltitol particles, mannitol particles, isomalt particles, and combinations thereof, in an amount of at least 60% by weight of the powder composition; and

ii) an ion-exchange composition in powder form for oromucosal delivery of nicotine, the ion-exchange composition comprising:

a plurality of particles consisting essentially of at least one polacrilex resin loaded with nicotine, the polacrilex resin loaded with nicotine being at least partly coated with at least one water-soluble anionic mucoadhesive polymer,

wherein the at least one water-soluble anionic mucoadhesive polymer is selected from sulfonated polysaccharides, anionic polysaccharides, polyacrylic acid, and combinations thereof,

wherein the at least one water-soluble anionic mucoadhesive polymer is operable to form a gel in contact with the oral mucosa when hydrated with saliva,

wherein the at least one water-soluble anionic mucoadhesive polymer is operable to protect the nicotine until adherence to the oral mucosa, and

wherein the weight ratio of the at least one water-soluble anionic mucoadhesive polymer to nicotine is from 2:1 to 20:1.