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Claims for Patent: 6,699,885

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Claims for Patent: 6,699,885

Title: Substituted benzimidazole dosage forms and methods of using same
Abstract:Disclosed herein are methods, kits, combinations, and compositions for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibiting agent (PPI) and a buffering agent in a pharmaceutically acceptable carrier.
Inventor(s): Phillips; Jeffrey O. (Ashland, MO)
Assignee: The Curators of the University of Missouri (Columbia, MO)
Application Number:10/054,350
Patent Claims: 1. A method of treating a gastric acid related disorder in a subject in need thereof, comprising: providing a solid pharmaceutical composition for oral administration to the subject, the composition consisting essentially of: (a) a therapeutically effective amount of at least one acid labile, substituted benzimidazole H.sup.+, K.sup.+ -ATPase proton pump inhibitor; (b) at least one buffering agent in an amount of about 0.1 mEq to about 2.5 mEq per mg proton pump inhibitor; and (c) one or more optional pharmaceutically acceptable excipients; and orally administering the pharmaceutical composition to the subject, wherein upon oral administration of the pharmaceutical composition to the subject, an initial serum concentration of the proton pump inhibitor greater than about 0.1 .mu.g/ml is obtained at any time within about 30 minutes after administration of the composition.

2. The method of claim 1, wherein the composition is administered in an amount to achieve an initial serum concentration of the proton pump inhibitor greater than about 0.15 .mu.g/ml at any time within about 30 minutes after administration of the composition.

3. The method of claim 1, wherein the pharmaceutical composition is in a form selected from the group consisting of a tablet, capsule, powder, suspension tablet, effervescent tablet or capsule, chewable tablet, granules, pellets, and a liquid created by mixing any of the foregoing with an aqueous medium.

4. The method of claim 1, wherein the amount of the proton pump inhibitor absorbed into the serum is therapeutically effective in treating the gastric acid related disorder selected from the group consisting of duodenal ulcer disease, gastric ulcer disease, gastroesophageal reflux disease, erosive esophagitis, poorly responsive symptomatic gastroesophageal reflux disease, pathological gastrointestinal hypersecretory disease, Zollinger Ellison Syndrome, heartburn, esophageal disorder, and acid dyspepsia.

5. The method of claim 1, wherein the proton pump inhibitor is selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, tautomer, ester, amide, derivative, prodrug, free base, or salt thereof.

6. The method of claim 1, wherein the amount of the proton pump inhibitor is about 2 mg to about 300 mg.

7. The method of claim 1, wherein the amount of the proton pump inhibitor is about 10 mg to about 120 mg.

8. The method of claim 1, wherein the amount of the proton pump inhibitor is about 2 mg, about 5 mg, about 10 mg, about 15 mg, about 20 mg, about 25 mg, about 30 mg, about 35 mg, about 40 mg, about 45 mg, about 50 mg, about 55 mg, about 60 mg, about 65 mg, about 70 mg, about 75 mg, about 80 mg, about 85 mg, about 90 mg, about 95 mg, about 100 mg, about 105 mg, about 110 mg, a 115 mg, or about 120 mg.

9. The method of claim 1, wherein the amount of the buffering agent is about 10 mEq to about 70 mEq.

10. The method of claim 1, wherein the amount of the buffering agent is at least 10 mEq.

11. The method of claim 1, wherein the amount of the buffering agent is about 15 mEq to about 55 mEq.

12. The method of claim 1, wherein the buffering agent comprises a combination of calcium carbonate and sodium bicarbonate.

13. The method of claim 1, wherein the buffering agent comprises a bicarbonate salt of a Group IA metal.

14. The method of claim 1, wherein the buffering agent is selected from the group consisting of a bicarbonate salt of a Group IA metal, an alkali earth metal buffering agent, a calcium buffering agent, a magnesium buffering agent, an aluminum buffering agent, sodium bicarbonate, potassium bicarbonate, magnesium hydroxide, magnesium lactate, magnesium gluconate, magnesium oxide, magnesium aluminate, magnesium carbonate, magnesium silicate, magnesium citrate, aluminum hydroxide, aluminum phosphate, aluminum hydroxide/magnesium carbonate, potassium carbonate, potassium citrate, aluminum hydroxide/sodium bicarbonate coprecipitate, aluminum glycinate, aluminum magnesium hydroxide, sodium citrate, sodium tartrate, sodium acetate, sodium carbonate, sodium polyphosphate, potassium polyphosphate, sodium pyrophosphate, sodium dihydrogen phosphate, potassium pyrophosphate, disodium hydrogenphosphate, dipotassium hydrogenphosphate, trisodium phosphate, tripotassium phosphate, potassium metaphosphate, calcium acetate, calcium glycerophosphate, calcium chloride, calcium hydroxide, calcium lactate, calcium carbonate, calcium gluconate, calcium bicarbonate, calcium citrate, calcium phosphate magnesium phosphate, potassium phosphate, sodium phosphate, trihydroxymethylaminomethane, an amino acid, an acid salt of an amino acid, an alkali salt of an amino acid, and combinations of any of the foregoing.

15. The method of claim 1, wherein the buffering agent comprises sodium bicarbonate.

16. The method of claim 15, wherein the sodium bicarbonate is in an amount from about 250 mg to about 4000 mg.

17. The method of claim 15, wherein the sodium bicarbonate is in an amount from about 1000 mg to about 2000 mg.

18. The method of claim 15, wherein the sodium bicarbonate is in an amount of at least about 400 mg.

19. The method of claim 1, wherein the buffering agent comprises calcium carbonate.

20. The method of claim 19, wherein the calcium carbonate is in an amount from about 250 mg to about 4000 mg.

21. The method of claim 19, wherein the calcium carbonate is in an amount from about 1000 mg to about 2000 mg.

22. The method of claim 19, wherein the calcium carbonate is in an amount of at least about 400 mg.

23. The method of claim 1, wherein the excipient is selected from the group consisting of a pharmaceutically compatible carrier, a binder, a suspending agent, a flavoring agent, a sweetening agent, a disintegrant, a flow aid, a lubricant, an adjuvant, a colorant, a diluent, a moistening agent, a preservative, a parietal cell activator, an anti-foaming agent, an antioxidant, a chelating agent, an antifungal agent, an antibacterial agent, e* an isotonic agent, and combinations of any of the foregoing.

24. The method of claim 1, wherein the excipient is one or more flavoring agents selected from the group consisting of aspartame, thaumatin, sucrose, dextrose, or a chocolate, a cocoa, a cola, a peppermint, a spearmint, a watermelon, an apple, a caramel, a meat, a root beer, a maple, a cherry, a coffee, a mint, a licorice, a nut, a butter, a butterscotch, a butter pecan, or a peanut butter flavoring, and combinations of any of the foregoing.

25. The method of claim 1, wherein the composition is administered once or twice a day.

26. A method of treating a gastric acid related disorder in a subject in need thereof, comprising: orally administering to the subject a single dose of a solution or suspension of a pharmaceutical composition, the composition consisting essentially of: (a) a therapeutically effective amount of at least one acid labile, substituted benzimidazole H.sup.+, K.sup.+ -ATPase proton pump inhibitor; (b) at least one buffering agent in an amount of about 0.1 mEq to about 2.5 mEq per mg proton pump inhibitor; and (c) one or more optional pharmaceutically acceptable excipients wherein an initial serum concentration of the proton pump inhibitor greater than about 0.1 .mu.g/ml is obtained at any time within about 30 minutes after administration of the composition, and wherein the administering step does not require further administration of the buffering agent(s) beyond that administered in the single dose.

27. The method of claim 26, wherein the composition is administered in an amount to achieve an initial serum concentration of the proton pump inhibitor greater than about 0.15 .mu.g/ml at any time within about 30 minutes after administration of the composition.

28. The method of claim 26, wherein the subject is fasting.

29. The method of claim 26, wherein the proton pump inhibitor is selected from the group consisting of omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, pariprazole, and leminoprazole, or an enantiomer, isomer, tautomer, ester, amide, derivative, prodrug, free base, or salt thereof.

30. The method of claim 26, wherein the amount of the proton pump inhibitor is about 2 mg to about 300 mg.

31. The method of claim 26, wherein the amount of the proton pump inhibitor is about 10 mg to about 120 mg.

32. The method of claim 26, wherein the amount of the proton pump inhibitor is about 2 mg, about 5 mg, about 10 mg, about 15 mg, about 20 mg, about 25 mg, about 30 mg, about 35 mg, about 40 mg, about 45 mg, about 50 mg, about 55 mg, about 60 rug, about 65 mg, about 70 mg, about 75 mg, about 80 mg, about 85 mg, about 90 mg, about 95 rug, about 100 mg, about 105 mg, about 110 mg, about 15 mg, or about 120 mg.

33. The method of claim 26, wherein the amount of the buffering agent is about 10 mEq to about 70 mEq.

34. The method of claim 26, wherein the amount of the buffering agent is at least 10 mEq.

35. The method of claim 26, wherein the amount of the buffering agent is about 15 mEq to about 55 mEq.

36. The method of claim 26, wherein the buffering agent comprises a combination of calcium carbonate and sodium bicarbonate.

37. The method of claim 26, wherein the buffering agent comprises a bicarbonate salt of a Group IA metal.

38. The method of claim 26, wherein the buffering agent is selected from the group consisting of a bicarbonate salt of a Group IA metal, an alkali earth metal buffering agent, a calcium buffering agent, a magnesium buffering agent, an aluminum buffering agent, sodium bicarbonate, potassium bicarbonate, magnesium hydroxide, magnesium lactate, magnesium gluconate, magnesium oxide, magnesium aluminate, magnesium carbonate, magnesium silicate, magnesium citrate, aluminum hydroxide, aluminum phosphate, aluminum hydroxide/magnesium carbonate, potassium carbonate, potassium citrate, aluminum hydroxide/sodium bicarbonate coprecipitate, aluminum glycinate, aluminum magnesium hydroxide, sodium citrate, sodium tartrate, sodium acetate, sodium carbonate, sodium (polyphosphate, sodium dihydrogen phosphate, potassium polyphosphate, sodium pyrophosphate, potassium pyrophosphate, disodium hydrogenphosphate, dipotassium hydrogenphosphate, trisodium phosphate, tripotassium phosphate, potassium metaphosphate, calcium acetate, calcium glycerophosphate, calcium chloride, calcium hydroxide, calcium lactate, calcium carbonate, calcium gluconate, calcium bicarbonate, calcium citrate, calcium phosphate magnesium phosphate, potassium phosphate, sodium phosphate, trihydroxymethylaminomethane, ail amino acid, an acid salt of an amino acid, an alkali salt of an amino acid, and combinations of any of the foregoing.

39. The method of claim 26, wherein the buffering agent comprises sodium bicarbonate.

40.The method of claim 39, wherein the sodium bicarbonate is in an amount from about 250 mg to about 4000 mg.

41. The method of claim 39, wherein the sodium bicarbonate is in an amount from about 1000 mg to about 2000 mg.

42. The method of claim 39, wherein the sodium bicarbonate is in an amount of at least about 400 mg.

43. The method of claim 39, wherein the buffering agent comprises calcium carbonate.

44. The method of claim 43, wherein the calcium carbonate is in an amount from about 250 mg to about 4000 mg.

45. The method of claim 43, wherein the calcium carbonate is in an amount from about 1000 mg to about 2000 mg.

46. The method of claim 43, wherein the calcium carbonate is in an amount of at least about 400 mg.

47. The method of claim 26, wherein the excipient is selected from the group consisting of a pharmaceutically compatible carrier, a binder, a suspending agent, a flavoring agent, a sweetening agent, a disintegrant, a flow aid, a lubricant, an adjuvant, a colorant, a diluent, a moistening agent, a preservative, a parietal cell activator, an anti-foaming agent, an antioxidant, a chelating agent, an antifungal agent, an antibacterial agent, or an isotonic agent, and combinations of any of the foregoing.

48. The method of claim 26, wherein the subject is an adult human.

49. The method of claim 26, wherein the disorder is selected from the group consisting of duodenal ulcer disease, gastric ulcer disease, gastroesophageal reflux disease, erosive esophagitis, poorly responsive symptomatic gastroesophageal reflux disease, pathological gastrointestinal hypersecretory disease, Zollinger Ellison Syndrome, heartburn, esophageal disorder, and acid dyspepsia.

50. The method of claim 26, wherein the excipient is one or more flavoring agents selected from the group consisting of aspartame, thaumatin, sucrose, dextrose, or a chocolate, a cocoa, a cola, a peppermint, a spearmint, a watermelon, an apple, a caramel, a meat, a root beer, a maple, a cherry, a coffee, a mint, a licorice, a nut, a butter, a butterscotch, a butter pecan, or a peanut butter flavoring, and combinations of any of the foregoing.

51. The method of claim 26, wherein the composition is administered once or twice a day.
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