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|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:||Jul 10, 2000|
|Claims:||1. A dosage form for delivery of a therapeutically effective amount of a drug to a target area in the gastrointestinal tract of a mammal; comprising: |
(a) a therapeutically effective amount of a drug;
(b) at least one effervescent penetration enhancer; wherein said at least one effervescent penetration enhancer is present in an amount sufficient to increase the penetration of said drug across said target area of said gastrointestinal tract to permit delivery of a therapeutically effective amount of said drug; and
(c) an enteric coating maintained over said drug and said at least one effervescent penetration enhancer; wherein said enteric coating prevents the release of said drug and said at least one effervescent penetration enhancer until a time at which said dosage form reaches said target area in said gastrointestinal tract.
2. The dosage form of claim 1, further comprising at least one noneffervescent penetration enhancer.
3. The dosage form of claim 1, further comprising at least one disintegration agent, wherein said disintegration agent causes the rapid dispersion of said drug to said target area of said gastrointestinal tract.
4. The dosage form of claim 1, wherein said enteric coating comprises a material that reacts with an enzyme present in said target area of the gastrointestinal tract to release said drug and said effervescent penetration enhancer.
5. The dosage form of claim 1, wherein said dosage form is a tablet.
6. The dosage from of claim 5 wherein said tablet contains a biconcave zone central to two outer zones; wherein said drug and said effervescent penetration enhancer are located in said biconcave zone.
7. The dosage form of claim 1, wherein said two outer zones contain a bioadhesive.
8. The dosage form of claim 1, wherein said effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple; said effervescent couple comprising an acid or equivalent thereof and a base or equivalent thereof.
9. The dosage form of claim 8 wherein said base is sodium bicarbonate.
10. The dosage form of claim 1 wherein said drug is a drug that displays poor bioavailability in said gastrointestinal tract.
11. The dosage form of claim 1, wherein said effervescent penetration enhancer comprises a pharmaceutically acceptable effervescent couple comprising an acid and a base, wherein said acid is selected from the group consisting of citric, tartaric, amalic, fumeric, adipic, and succinic acids, and said base is selected from the group consisting of sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate and magnesium carbonate.
12. The dosage form of claim 2, further comprising a noneffervescent disintegration agent.
13. The dosage form of claim 2, wherein said protective coating comprises a material that reacts with an enzyme present in said area of the gastrointestinal tract to release said drug, said effervescent penetration enhancer and said noneffervescent penetration enhancer.
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