JP2008500365A5

JP2008500365A5 -

Info

Publication number: JP2008500365A5
Application number: JP2007515351A
Authority: JP
Filing date: 2005-05-25
Publication date: 2008-05-08

Claims

A tablet oral dosage form pharmaceutical formulation comprising:
(a) about 10 mg to about 100 mg of at least one bicyclic aryl-imidazolic acid labile proton pump inhibitor;
(b) about 400 mg to about 1400 mg of NaHCO _3Three ;
(c) from about 2% to about 8% by weight of a disintegrant; and
(d) about 3% to about 10% by weight binder;
Here, during oral administration of tablets to fasting subjects, the proton pump inhibitor T _maxmax A pharmaceutical formulation obtained within about 45 minutes after administration on the first day.

The tablet further comprises an antacid selected from potassium bicarbonate, sodium carbonate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, aluminum hydroxide, and mixtures thereof and present in the tablet. 3. The pharmaceutical formulation of claim 2, wherein the total amount of acid agent is from about 10 mEq to about 30 mEq.

The pharmaceutical formulation of claim 1, wherein the sodium bicarbonate is present in an amount of at least about 700 mg.

2. The pharmaceutical formulation of claim 1, wherein the disintegrant is present in an amount of about 3% to about 5% by weight.

Binding agent is present in an amount of about 5 wt% to about 8 wt%, pharmaceutical formulation of claim 1, wherein.

The pharmaceutical of claim 1 , wherein upon administration of the tablet to the subject, the initial serum concentration of the proton pump inhibitor is greater than about 300 ng / ml within about 45 minutes after oral administration of the tablet to the subject. Formulation.

The pharmaceutical formulation of claim 1, consisting essentially of:
(a) omeprazole, esomeprazole, lansoprazole, or a salt thereof in an amount of about 20 mg or about 40 mg;
(b) about 700 mg to about 1400 mg of NaHCO _3Three ;
(c) from about 2% to about 8% by weight of a disintegrant;
(d) about 3% to about 10% by weight of a binder; and
(e) About 0.5% and about 3% by weight lubricant.

NaHCO _3Three Is present in an amount of about 1100 mg to 1400 mg; the disintegrant is croscarmellose sodium and is present in an amount of about 3% to about 5% by weight; and the binder is hydroxypropylcellulose; and about 5 The pharmaceutical formulation according to claim 7, present in an amount of from about 10% to about 10% by weight of the proton pump inhibitor T during oral administration of the tablet to a fasting subject. _maxmax A pharmaceutical formulation obtained within about 45 minutes after administration on the first day.

A pharmaceutical formulation in a capsule dosage form comprising:
(a) about 10 mg to about 100 mg of at least one bicyclic aryl-imidazolic acid labile proton pump inhibitor;
(b) about 400 mg to about 1400 mg of NaHCO ₃ ; and
(c) from about 2% to about 5% by weight of a disintegrant ;
A pharmaceutical formulation wherein the _Tmax of the proton pump inhibitor is obtained within about 60 minutes after administration on day 1 upon oral administration of the capsule to a fasting subject .

The capsule further comprises an antacid selected from potassium bicarbonate, sodium carbonate, calcium carbonate, magnesium oxide, magnesium hydroxide, magnesium carbonate, aluminum hydroxide, and mixtures thereof and is present in the capsule. 10. The pharmaceutical formulation of claim 9 , wherein the total amount of acid agent is from about 10 mEq to about 30 mEq .

The pharmaceutical formulation of claim 9 , wherein the sodium bicarbonate is present in an amount of at least about 800 mg.

10. The pharmaceutical formulation of claim 9 , wherein the disintegrant is present in an amount of about 3 % to about 5 % by weight.

10. The pharmaceutical formulation of claim 9 , wherein the day 7 T _max of the proton pump inhibitor is obtained within about 60 minutes after oral administration of the capsule to the subject.

The pharmaceutical formulation of claim 9, consisting essentially of:
(a) omeprazole or a salt thereof in an amount of about 20 mg or about 40 mg;
(b) about 800 mg to about 1400 mg of NaHCO _3Three ;
(c) from about 2% to about 8% by weight of a disintegrant; and
(e) About 0.5 wt% to about 3 wt% lubricant.

NaHCO _3Three 15. The pharmaceutical composition of claim 14, wherein is present in an amount of about 1000 mg to 1300 mg; and the disintegrant is croscarmellose sodium and is present in an amount of about 3% to about 5% by weight. When the capsule is administered orally to a fasting subject, the proton pump inhibitor T _maxmax Wherein the pharmaceutical composition is obtained within about 60 minutes after administration on the first day.