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Claims for Patent: 6,645,988

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Claims for Patent: 6,645,988

Title: Substituted benzimidazole dosage forms and method of using same
Abstract:The present invention relates to pharmaceutical preparations comprising substituted benzimidazole proton pump inhibitors. There is provided a liquid or solid pharmaceutical dosage form that is not enteric coated or delayed released containing a proton pump inhibitor and a Primary Essential Buffer. When the dosage form is placed in a liquid phase the Primary Essential Buffer maintains the pH of the environment at a value greater than the pKa of the proton pump inhibitor for a time sufficient to substantially avoid acid degradation of the proton pump inhibitor in the environment. Also provided is a method for treating acid-related gastrointestinal disorders by administering a solid pharmaceutical dosage form; and a kit for the preparation of a liquid oral pharmaceutical composition.
Inventor(s): Phillips; Jeffrey O. (Ashland, MO)
Assignee: Curators of the University of Missouri (Columbia, MO)
Application Number:09/901,942
Patent Claims: 1. A solid oral pharmaceutical dosage form that is not enteric-coated, comprising: active ingredients consisting essentially of: (a) at least one proton pump inhibitor (PPI) selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, and an enantiomer, isomer, free base, or salt thereof, in an amount of approximately 5 mg to approximately 300 mg; and (b) at least one Primary Essential Buffer and at least one optional Secondary Essential Buffer in a total amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor; and a pharmaceutically-acceptable excipient; wherein the dosage form is selected from the group consisting of a suspension tablet, chewable tablet, two-part tablet, effervescent powder, and effervescent tablet.

2. The dosage form of claim 1, wherein the proton pump inhibitor is in an amount from approximately 10 mg to approximately 100 mg.

3. The dosage form of claim 1, wherein the proton pump inhibitor is omeprazole.

4. The dosage form of claim 1, wherein the proton pump inhibitor is lansoprazole.

5. The dosage form of claim 1, wherein the proton pump inhibitor is pantoprazole.

6. The dosage form of claim 1, wherein the proton pump inhibitor is rabeprazole.

7. The dosage form of claim 1, wherein the proton pump inhibitor is esomeprazole.

8. The dosage form of claim 1, wherein the proton pump inhibitor is pariprazole.

9. The dosage form of claim 1, wherein the proton pump inhibitor is leminoprazole.

10. The dosage form of claim 1, wherein the Primary Essential Buffer is selected from the group consisting of sodium bicarbonate, sodium sesquicarbonate, dibasic sodium phosphate, sodium tripolyphosphate, tetrasodium pyrophosphate, sodium citrate, calcium citrate, calcium carbonate, magnesium oxide, sodium gluconate, sodium lactate, sodium acetate, dipotassium phosphate, tetrapotassium pyrophosphate, potassium bicarbonate, calcium lactate, calcium glycerophosphate, calcium gluconate, magnesium lactate, magnesium gluconate, and magnesium hydroxide, and mixtures thereof.

11. The dosage form of claim 10, wherein the Primary Essential Buffer is sodium bicarbonate.

12. The dosage form of claim 11, wherein the sodium bicarbonate is in an amount from about 400 mg to about 4000 mg.

13. The dosage form of claim 11, wherein the sodium bicarbonate is in an amount of at least about 800 mg.

14. The dosage form of claim 10, wherein the Primary Essential Buffer is calcium carbonate.

15. The dosage form of claim 14, wherein the calcium carbonate is in an amount from about 400 mg to about 4000 mg.

16. The dosage form of claim 14, wherein the calcium carbonate is in an amount from about 500 mg to about 1000 mg.

17. The dosage form of claim 14, wherein the calcium carbonate is in an amount of at least about 700 mg.

18. The dosage form of claim 1, wherein the Secondary Essential Buffer is selected from the group consisting essentially of sodium carbonate, potassium carbonate, trisodium phosphate, tripotassium phosphate, calcium hydroxide, and sodium hydroxide.

19. The dosage form of claim 1, wherein the pharmaceutically-acceptable excipient comprises at least one flavoring agent.

20. The dosage form of claim 19, wherein the flavoring agent compnses apple, caramel, meat, chocolate, root beer, maple, cherry, coffee, mint, licorice, nut, butter, butterscotch, peanut butter, aspartame, chocolate, thalmantin, root beer, peppermint, spearmint, or watermelon, and combinations of any of the foregoing.

21. The dosage form of claim 1, wherein the pharmaceutically-acceptable excipient comprises an anti-foaming agent.

22. The dosage form of claim 1, wherein the pharmaceutically-acceptable excipient comprises a binder, diluent, lubricant, disintegrant, colorant, antioxidant, chelating agent, anti-caking agent, moistening agent, preservative, or coating.

23. The dosage form of claim 10, wherein the Primary Essential Buffer is sodium bicarbonate and calcium carbonate.

24. A solid oral pharmaceutical dosage form that is not enteric-coated, comprising: an outer layer and an inner core; the outer layer comprising active ingredients consisting essentially of at least one Primary Essential Buffer; and the inner core comprising active ingredients consisting essentially of at least one proton pump inhibitor selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, free base, or salt thereof, and at least one buffering agent selected from the group consisting of a Primary Essential Buffer and a Secondary Essential Buffer; wherein the total amount of the proton pump inhibitor is approximately 5 mg to approximately 300 mg; and the total amount of the buffering agent is approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor.

25. A method of administering the dosage form of claim 1, comprising: orally administering the dosage form to a subject, wherein the amount of the Primary Essential Buffer and the optional Secondary Essential Buffer is effective to elevate pH of gastric fluid of the subject upon oral administration to at least 3.7 from time the proton pump inhibitor comes in contact with the gastric fluid throughout dwell time in the stomach.

26. The method of claim 25, wherein the amount of the Primary Essential Buffer and the optional Secondary Essential Buffer is effective to elevate the pH of the gastric fluid of the subject upon oral administration to at least 4.6.

27. The method of claim 25, wherein the amount of the Primary Essential Buffer and the optional Secondary Essential Buffer is effective to elevate the pH of the gastric fluid of the subject upon oral administration to at least 4.8.

28. The method of claim 25, wherein the amount of the Primary Essential Buffer and the optional Secondary Essential Buffer is effective to elevate the pH of the gastric fluid of the subject upon oral administration to at least 5.6.

29. A non-enteric coated solid oral pharmaceutical dosage form, comprising: (a) active ingredients consisting essentially of: (i) a proton pump inhibitor (PPI) selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, and an enantiomer, isomer, free base, and salt thereof, in an amount of approximately 5 mg to approximately 300 mg; and (ii) at least one Primary Essential Buffer and at least one optional Secondary Essential Buffer in a total amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of proton pump inhibitor; and (b) a pharmaceutically-acceptable excipient;

wherein the dosage form is created by a method comprising: i) blending the proton pump inhibitor, the Primary Essential Buffer, the optional Secondary Essential Buffer, and the pharmaceutically-acceptable excipient; and ii) formulating the proton pump inhibitor, the Primary Essential Buffer, the optional Secondary Essential Buffer, and the pharmaceutically-acceptable excipient into a powder, tablet, suspension tablet, chewable tablet, capsule, two-part tablet, two-part capsule, effervescent powder, pellet, granule or effervescent tablet.
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