Compositions and Methods for Inhibiting Gastric Acid Secretion

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 one or more small carboxylic acid molecules or any salts thereof which activate parietal cells, wherein the small carboxylic acid molecules or any salts thereof are saturated or non-saturated monocarboxylic, dicarboxylic or tricarboxylic acid molecules or any salts thereof involved in the mitochondrial respiration circle (krebs cycle) having between three to six carbon atoms selected from the group consisting of maleic acid, citric acid, pyruvate, fumarate, alpha-ketoglutarate, succinyl-CoA and oxaloacetate;
• 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 molecules or any salts thereof in the stomach, the PPI is enteric-coated and is formulated for absorption in the small intestine and the carboxylic acid molecules or any salts thereof are 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 molecules or any salts thereof being between 50 to 2500 mg, wherein the carboxylic acid molecules or any salts thereof in conjunction with the PPI reduces 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 one or more small carboxylic acid molecules or any salts thereof which activate parietal cells, wherein the small carboxylic acid molecules or any salts thereof are saturated or non-saturated monocarboxylic, dicarboxylic or tricarboxylic acid molecules or any salts thereof involved in the mitochondrial respiration circle (krebs cycle) having between three to six carbon atoms selected from the group consisting of maleic acid, citric acid, pyruvate, fumarate, alpha-ketoglutarate, succinyl-CoA and oxaloacetate;
• 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 molecules or any salts thereof in the stomach, the carboxylic acid molecules or any salts thereof 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 molecules or any salts thereof being between 50 to 2500 mg, wherein the carboxylic acid molecules or any salts thereof in conjunction with the PPI reduces gastric acid secretion in the human patient.

A pharmaceutical composition in a solid dosage form suitable for oral 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 one or more small carboxylic acid molecules or any salts thereof which activate parietal cells, wherein the small carboxylic acid molecules or any salts thereof are saturated or non-saturated monocarboxylic, dicarboxylic or tricarboxylic acid molecules or any salts thereof involved in the mitochondrial respiration circle (krebs cycle) having between three to six carbon atoms selected from the group consisting of maleic acid, citric acid, pyruvate, fumarate, alpha-ketoglutarate, succinyl-CoA and oxaloacetate;

• 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, pro-drugs thereof, and mixtures thereof, wherein the small carboxylic acid molecules or any salts thereof are in a form for release in the stomach in an amount of between 50 to 2500 mg 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 molecules or any salts thereof enhance the activity of the PPI at inhibiting gastric acid secretion in the stomach.