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US 7,803,817 B2Granted
Composition and methods for inhibiting gastric acid secretion
AssigneeVecta, Ltd.
InventorsAleksey Kostadinov, Ayelet David, Sabina Glozman
Life of this patent
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Abstract
The present invention is related to oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and succinc acid as a parietal cell activator in the gastric lumen. The compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.
Claims22
A pharmaceutical composition in a solid dosage form selected from the group consisting of:
- capsules and tablets, wherein the active ingredients of said composition consist of a pharmaceutically effective amount of:
- (i) a parietal cell activator, wherein the parietal cell activator is a small carboxylic acid molecule which activates parietal cells, wherein the small carboxylic acid molecule is succinic acid or a salt thereof;
- and (ii) an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI), wherein the capsule or tablet solid dosage form is suitable for administration to a human patient, wherein the capsule or tablet solid dosage form disintegrates in the stomach and the release of the active ingredients is controlled such that the activity of the PPI is synchronized with the parietal cell activity of the carboxylic acid molecule in the stomach, the PPI is enteric-coated and formulated for absorption in the small intestine and the carboxylic acid molecule is in a form for release in the stomach in an amount sufficient to activate parietal cells located in the gastric lumen of the human patient so that the parietal cells are active while the PPI is in the patient's blood having been absorbed through the small intestine, the amount of the small carboxylic acid molecule being between 50 to 2500 mg, wherein the carboxylic acid molecule in conjunction with the PPI reduces gastric acid secretion in the stomach.
A pharmaceutical kit for administration to a human patient wherein the active ingredients consist of a pharmaceutically effective amount of:
- (i) a parietal cell activator, wherein the parietal cell activator is a small carboxylic acid molecule which activates parietal cells, wherein the small carboxylic acid molecule is, succinic acid or a salt thereof;
- and (ii) an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI), wherein the kit comprises a solid capsule and/or tablet dosage form suitable for administration to a human patient that disintegrate in the stomach and the release of the active ingredients is controlled such that the activity of the PPI is synchronized with the parietal cell activity of the carboxylic acid molecule in the stomach, the PPI is enteric-coated and is formulated for absorption in the small intestine and the carboxylic acid molecule is in a form for release in the stomach in an amount sufficient to activate parietal cells located in the gastric lumen of the human patient so that the parietal cells are active while the PPI is in the patient's blood having been absorbed through the small intestine, the amount of the small carboxylic acid molecule being between 50 to 2500 mg, wherein the carboxylic acid molecule in conjunction with the PPI reduces gastric acid secretion in the stomach.
A pharmaceutical composition in a solid dosage form selected from the group consisting of:
- capsules and tablets suitable for administration to a human patient, wherein the active ingredients of the capsules and tablets consist of a pharmaceutically effective amount of:
- (i) a parietal cell activator, wherein the parietal cell activator is a small carboxylic acid molecule which activate parietal cells, wherein the small carboxylic acid molecules is succinic acid or a salt thereof;
- and (ii) an enteric-coated irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) selected from the group consisting of:
- rabeprazole, omeprazole, isomeprazole, lansoprazole, pantoprazole, leminoprazole, tenatoprazole, single enantiomers thereof, alkaline salts thereof and mixtures thereof, wherein the small carboxylic acid molecule is in a form for release in the stomach in an amount of between 50 to 2500 mg so that the parietal cell located in the gastric lumen of the human patient are active while the PPI is in the patient's blood wherein the carboxylic acid molecule enhances the activity of the PPI at inhibiting gastric acid secretion in the stomach.
1 more element
A pharmaceutical composition in a solid dosage form selected from the group consisting of:
- capsules and tablets suitable for administration to a human patient, wherein the active ingredients of the capsules and tablets consist of a pharmaceutically effective amount of:
- (i) a parietal cell activator, wherein the parietal cell activator is a small carboxylic acid molecule which activates parietal cells, wherein the small carboxylic acid molecules is succinic acid or a salt thereof;
- and (ii) an enteric-coated irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI), wherein the weight ratio between the carboxylic acid molecules or any salts thereof and the PPI is about 20:1 to 1:5 and the carboxylic acid molecule is in a form for release in the stomach so that the parietal cells located in the gastric lumen of the human patient are active while the PPI is in the patient's blood, wherein the carboxylic acid molecule enhances the activity of the PPI at inhibiting gastric acid secretion in the stomach.
A method of reducing gastric acid secretion in a human patient, the method comprising administering to the patient an effective amount of a pharmaceutical composition in a solid dosage form selected from the group consisting of:
- capsules and tablets suitable for administration to a human patient, wherein the active ingredients of said composition consist of a parietal cell activator, wherein the parietal cell activator is a small carboxylic acid molecule which activates parietal cells, wherein the small carboxylic acid molecule is succinic acid or a salt thereof;
- and an effective amount of an enteric-coated proton pump inhibitor (PPI), wherein the tablet or capsule solid dosage form disintegrates in the stomach and the release of the active ingredient is controlled such that the activity of the PPI is synchronized with the parietal cell activity of the carboxylic acid molecule in the stomach, the carboxylic acid molecule being in a form for release in the stomach in an amount sufficient to activate parietal cells located in the gastric lumen of the human patient so that the parietal cells are active while the PPI is in the patient's blood having been absorbed through the small intestine, the amount of the small carboxylic acid molecule being between 50 to 2500 mg, wherein the carboxylic acid molecule in conjunction with the PPI reduces gastric acid secretion in the human patient.
Dependencies are inferred from the claim text.