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Details for Patent: 8,802,130

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Details for Patent: 8,802,130

Title: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.
Inventor(s): Pather; S. Indiran (Plymouth, MN), Khankari; Rajendra K. (Maple Grove, MN), Eichman; Jonathan D. (Pomona, NY), Robinson; Joseph R. (Madison, WI), Hontz; John (Plymouth, MN)
Assignee: Cephalon, Inc. (Frazer, PA)
Filing Date:Aug 28, 2006
Application Number:11/511,098
Claims:1. A method of manufacturing a compressed tablet suitable for direct oral administration across the oral mucosa, said method comprising the steps of: a) providing an amount of a salt of fentanyl that is pharmaceutically effective for systemic distribution and for oral mucosal administration; b) providing at least one saliva activated effervescent couple in an amount that is effective 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 95% by weight; c) producing a mixture from said pharmaceutically effective amount of a composition consisting of a salt of fentanyl 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 at least one saliva activated effervescent couple is present in an amount between about 20% by weight and 80% by weight.

6. The method according to claim 1, wherein said at least one effervescent couple is present in an amount between about 5% by weight to about 80% by weight.

7. The method according to claim 1, wherein said at least one effervescent couple is present in an amount sufficient to evolve a gas in an amount between about 5 cm.sup.3 to about 30 cm.sup.3.

8. The method according to claim 1, wherein said mixture further comprises a pH adjusting substance.

9. The method according to claim 8, wherein said pH adjusting substance is a base and 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.

10. The method according to claim 1 further comprising the step of 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 and producing said mixture including same.

11. The method according to claim 10, wherein said pH adjusting substance is a base.

12. The method according to claim 11, 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.

13. 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 consisting of a salt of fentanyl, capable of existing in an ionized form and a unionized form in aqueous environment; b) providing a pharmaceutically effective amount for systemic distribution and for oral mucosal administration of said at least one orally administrable medicament; c) selecting at least one saliva activated effervescent couple; d) selecting a basic pH adjusting substance in an amount 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; e) producing a mixture from said medicament, said selected saliva activated effervescent couple and said pH adjusting substance, in said predetermined amounts; and f) compressing at least a portion of said mixture so as to form at least one tablet.

14. The method according to claim 13, wherein said basic pH adjusting substance 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.

15. The method of claim 13 further comprising the step of selecting a bioadhesive and producing said mixture including same.

16. The method of claim 13 wherein said amount of said at least one effervescent couple ranges from about 5% by weight to about 80% by weight.

17. The method of claim 13, further comprising the step of: selecting one or more glidants, lubricants, binders, sweeteners, flavoring and coloring components and producing said mixture including same.

18. 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 consisting of a salt of fentanyl, capable of existing in an ionized form and a unionized form in aqueous environment; b) providing a pharmaceutically effective amount for systemic distribution and for oral mucosal administration of said at least one orally administrable medicament; c) selecting at least one saliva activated effervescent couple in an amount of from about 5% by weight to about 80% by weight; d) selecting a basic pH adjusting substance from the group consisting of sodium carbonate, potassium carbonate, magnesium carbonate, disodium hydrogen phosphate, sodium dihydrogen phosphate, dipotassium hydrogen phosphate, and potassium dihydrogen phosphate, in an amount 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; e) selecting a bioadhesive substance suitable for use in the oral cavity; f) selecting one or more excipient from the group consisting of glidants, lubricants, binders, sweeteners, flavoring and coloring components; g) producing a mixture from said medicament, said selected saliva activated effervescent couple, said pH adjusting substance, said bioadhesive; and said excipient; and h) compressing at least a portion of said mixture so as to form at least one tablet.

19. The tablet produced by the method of claim 1.

20. The tablet produced by the method of claim 14.

21. The tablet produced by the method of claim 15.

22. The tablet produced by the method of claim 13.

23. The tablet produced by the method of claim 18.

24. The method of claim 1, wherein the salt of fentanyl comprises fentanyl citrate.

25. The method of claim 13, wherein the salt of fentanyl comprises fentanyl citrate.

26. The method of claim 18, wherein the salt of fentanyl comprises fentanyl citrate.
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