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Details for Patent: 6,509,036

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Details for Patent: 6,509,036

Title: Effervescent drug delivery system for oral administration
Abstract:The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.
Inventor(s): Pather; S. Indiran (Plymouth, MN), Robinson; Joseph R. (Madison, WI), Eichman; Jonathan D. (Ann Arbor, MI), Khankari; Rajendra K. (Maple Grove, MN), Hontz; John (Plymouth, MN), Gupte; Sangeeta V. (Maple Grove, MN)
Assignee: Cima Labs Inc. (Minneapolis, MN)
Filing Date:Oct 29, 2001
Application Number:10/021,486
Claims:1. A method for delivering a drug to a target area of the gastrointestinal tract of a mammal, said method comprising the steps of: (a) orally administering a dosage form comprising a therapeutically effective amount of a drug and at least one effervescent penetration enhancer in an amount sufficient to increase the penetration of said drug across said target area to permit absorption of said therapeutically effective amount of said drug, said amount of said effervescent penetration enhancer being greater than an amount necessary for rapid disintegration of said dosage form at said target area; (b) causing said drug and said effervescent penetration enhancer to release from said dosage form at said target area and to provide effervescent action at said target area thereby said effervescent action promotes said absorption of said therapeutically effective amount of said drug across said target area by said increased penetration of said drug across said target area.

2. The method of claim 1, wherein said amount of said at least one effervescent penetration enhancer is at least about two times the amount of said drug.

3. The method of claim 2, wherein said amount of said at least one effervescent penetration enhancer is equal about two times the amount of said drug.

4. The method of claim 2, wherein said amount of said at least one effervescent penetration enhancer is at least about three times the amount of said drug.

5. The method of claim 4, wherein said amount of said at least one effervescent penetration enhancer is equal about three times the amount of said drug.

6. The method of claim 2, wherein said at least one effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple; said effervescent couple comprising an acid or equivalent thereof and a base or equivalent thereof.

7. The method of claim 6, wherein said base or equivalent thereof is present in an amount equal to or greater than about two times the amount of said drug; and said acid is present in an amount approximately equimolar to said base.

8. The method of claim 7, wherein said base or equivalent thereof is present in an amount equal to or greater than about three times the amount of said drug.

9. The method of claim 1, wherein said dosage form further comprises a material for site-specific delivery of said drug, wherein said material is selected from the group consisting of coatings and matrix materials.

10. The method of claim 9, wherein said target area is selected from the group consisting of stomach, duodenum, intestines, and the colon.

11. The method of claim 1, wherein said dosage form further comprises one or more ingredients selected from the group consisting of pH-adjusting substance, non-effervescent penetration enhancers, bioadhesives, and disintegration agents.

12. A method of manufacturing a pharmaceutical composition that comprises a drug absorbed through a transmucosal route at a target area of a gastrointestinal tract of a mammal, said method comprising the steps of: a) combining a pharmaceutically effective amount of said drug with an effervescent penetration enhancer to produce a mixture; b) coating said mixture with an enteric coating thereby providing a dosage form;

wherein said effervescent penetration enhancer is present in an amount greater than an amount necessary for rapid disintegration of said dosage form.

13. The method of claim 12, wherein said mixture comprises layers of said drug and said effervescent penetration enhancer.

14. The method of claim 12, wherein said mixture further comprises a liquid.

15. The method of the claim 12, wherein said dosage form is selected from the groups consisting of a tablet, granules, pellets, and a capsule.

16. The method of claim 12, wherein said mixture comprises said drug in the form of minitablets, beads, or powder.

17. The method of claim 12, wherein said dosage form is manufactured by wet granulation, dry granulation, or direct compression.

18. The method of claim 12, wherein said mixture said mixture further comprises one or more excipient fillers.

19. The method of claim 18, wherein said excipient fillers are selected from the group consisting of mannitol, dextrose, lactose, sucrose, and calcium carbonate.

20. The method of claim 12, wherein said amount of said at least one effervescent penetration enhancer is at least about two times the amount of said drug.

21. The method of claim 20, wherein said amount of said at least one effervescent penetration enhancer is equal about two times the amount of said drug.

22. The method of claim 12, wherein said amount of said at least one effervescent penetration enhancer is at least about three times the amount of said drug.

23. The method of claim 22, wherein said amount of said at least one effervescent penetration enhancer is equal about three times the amount of said drug.

24. The method of claim 12, wherein said at least one effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple; said effervescent couple comprising an acid or equivalent thereof and a base or equivalent thereof.

25. The method of claim 24, wherein said base or equivalent thereof is present in an amount equal to or greater than about two times the amount of said drug; and said acid is present in an amount approximately equimolar to said base.

26. The method of claim 25, wherein said base or equivalent thereof is present in an amount equal to or greater than about three times the amount of said drug.

27. The method of claim 12, wherein said target area is selected from the group consisting of stomach, duodenum, intestines, and the colon.

28. The method of claim 12, wherein said dosage form further comprises one or more ingredients selected from the group consisting of pH-adjusting substance, non-effervescent penetration enhancers, bioadhesives, and disintegration agents.
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