Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them

1. A pharmaceutical formulation in a single capsule dosage form consisting of:

(a) about 10 mgs to about 100 mgs of at least one micronized bicyclic aryl-imidazole acid-labile proton pump inhibitor;

(b) at least one antacid, wherein the antacid comprises about 400 mgs to about 1400 mgs of sodium bicarbonate;

(c) about 2 wt-% to about 5 wt-% of a disintegrant; and

(d) about 0.5 wt-% to about 3 wt-% of Magnesium Stearate

wherein upon oral administration of the capsule to a fasted human subject, a T max of the proton pump inhibitor is obtained within 60 minutes after administration on day 1; and an initial serum concentration of the proton pump inhibitor is greater than 300 ng/ml within 45 minutes after administration.

2. The pharmaceutical formulation according to claim 1 , wherein the proton pump inhibitor is omeprazole, esomeprazole or lansoprazole, or a salt thereof.

3. The pharmaceutical formulation according to claim 1 , wherein the antacid further comprises potassium bicarbonate, sodium carbonate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, aluminum hydroxide, or mixtures thereof; and the total amount of antacid present in the capsule is about 10 mEq.

4. The pharmaceutical formulation according to claim 1 , wherein the sodium bicarbonate is present in an amount of at least 800 mgs.

5. The pharmaceutical formulation according to claim 1 , wherein the disintegrant is croscarmellose sodium and is present in an amount of about 3 wt-%.

6. The pharmaceutical formulation according to claim 1 , wherein the disintegrant is present in an amount of about 3 wt-% to about 5 wt-%.

7. The pharmaceutical formulation of claim 1 , wherein T max of the proton pump inhibitor on day 7 is obtained within 60 minutes after oral administration of the capsule to the subject.

8. The pharmaceutical formulation according to claim 1 , wherein the average C max of the proton pump inhibiting agent is less than 1250 ng/ml after oral administration of the capsule to the subject.

9. A pharmaceutical formulation in a single capsule oral dosage form consisting of:

(a) micronized omeprazole or a salt thereof in an amount of about 20 mgs or about 40 mgs;

(b) about 800 mgs to about 1400 mgs of sodium bicarbonate (NaHCO 3 );

(c) about 2 wt-% to about 8 wt-% of a disintegrant; and

(d) about 0.5 wt-% to about 3 wt-% of Magnesium Stearate.

10. The pharmaceutical composition of claim 9 , wherein:

(a) the NaHCO 3 is present in an amount of between 1000 mgs and 1300 mgs; and

(b) the disintegrant is croscarmellose sodium and is present in an amount of about 3 wt-% to about 5 wt-%;

wherein upon oral administration of the capsule to a fasted human subject, a T max of the proton pump inhibitor is obtained within 60 minutes after administration on day 1.

11. A method of inhibiting a gastric acid related gastrointestinal disorder in a subject comprising administering one or more capsules of a single capsule oral dosage form to a human subject in need thereof, the single capsule oral dosage form consisting of:

(a) about 10 mgs to about 100 mgs of at least one micronized bicyclic aryl-imidazole acid-labile proton pump inhibitor;

(b) an antacid, wherein the antacid comprises about 400 mgs to about 1400 mgs of sodium bicarbonate (NaHCO 3 );

(c) about 2 wt-% to about 5 wt-% of a disintegrant; and

(d) about 0.5 wt-% to about 3 wt-% of Magnesium Stearate

wherein upon oral administration of the capsule to a fasted human subject, a Tmax of the proton pump inhibitor is obtained within 60 minutes after administration on day 1.