|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 administerable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of additional pH adjusting substance in combination with the effervescent for promoting the absorption of drugs is also disclosed.|
|Inventor(s):||Eichman; Jonathan D. (Ann Arbor, MI), Hontz; John (Plymouth, MN), Khankari; Rajendra K. (Maple Grove, MN), Pather; Sathasivan Indiran (Plymouth, MN), Robinson; Joseph R. (Madison, WI)|
|Assignee:||Cephalon, Inc. (Frazer, PA)|
1. A tablet comprising: a) fentanyl and/or at least one pharmaceutically acceptable salt thereof in a pharmaceutically effective amount for buccal mucosal administration in
a human; b) at least one effervescent couple present in an amount ranging from about 5% by weight to about 80% by weight based on the weight of the tablet, said effervescent couple comprising at least one acid and at least one base, wherein said at
least one base, which may be the same as or different from said at least one pH adjusting base, is present in an amount required for effervescence, wherein the at least one acid is selected from citric, tartaric, malic, fumaric, adipic and succinic acid,
and the at least one base is selected from sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate and magnesium carbonate; and c) at least one pH adjusting base, selected from sodium carbonate, potassium carbonate, magnesium
carbonate, disodium hydrogen phosphate, sodium dihydrogen phosphate, dipotassium hydrogen phosphate, and potassium dihydrogen phosphate, said pH adjusting base being present in an amount additional to that required for effervescence; and wherein said
tablet further comprises at least one disintegration agent present in an amount up to about 20% by weight based on the weight of the tablet.
2. The tablet according to claim 1, wherein said at least one disintegration agent is chosen from microcrystalline cellulose, croscarmelose sodium, crospovidone, starches, modified starches, sweeteners, clays, alginates, and gums.
3. The tablet according to claim 1, wherein the at least one disintegration agent is present in an amount ranging from 2% by weight to about 10% by weight based on the weight of the tablet.
4. The tablet according to claim 1, further comprising at least one additional component chosen from glidants, lubricants, binders, sweeteners, flavoring components, and coloring components.
5. The tablet according to claim 1, further comprising at least one bioadhesive.
6. The tablet according to claim 1, comprising fentanyl citrate.
7. A tablet according to claim 1, wherein: the at least one pH adjusting substance comprises sodium carbonate; at least one acid in the at least one effervescent couple comprises citric acid; and the at least one base in the at least one effervescent couple comprises sodium bicarbonate; and wherein the at least one disintegration agent comprises at least one modified starch.