57 results about "Gastric Acid Secretion Inhibition" patented technology

An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid susceptible proton pump inhibitor or a salt thereof, an H2 receptor antagonist or a salt thereof and a pharmaceutically acceptable carrier. The dosage form is capable of raising gastric pH to above 4 within two hours after administration and to keep it at that level for at least 4 hours. Also disclosed is a method of manufacture of the dosage form, its use in treating dyspepsia and infection by Helicobacter pylori, and a method of treating disorders associated with gastric acid secretion.

The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same.Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula:(wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4 represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.

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.

The present invention relates to a pyrrole sulfonamide derivative, a preparation method and a medical application thereof. Concretely, the present invention relates to the pyrrole sulfonamide derivative shown in a formula (I), the preparation method for the derivative, a pharmaceutical composition comprising the derivative, and uses of same as therapeutic agents, and particularly as a gastric acid secretion inhibitor and potassium-competitive acid blockers (P-CABs), where each substituent of formula (I) is as defined in the description.

The invention discloses a compound or its salt shown in the formula (I) and usage of the compound as a potassium competitive acid blocker or a gastric acid secretion inhibitor. The compound has a proton pump (H+ / K+)-ATPase inhibitory effect and can be used for preventing, treating and inhibiting diseases related to gastric acid secretion, such as peptic ulcer, zollinger-ellison syndromes, gastritis, erosive esophagitis, reflux esophagitis and symptomatic gastroesophageal reflux diseases.

The present invention is related to novel oral compositions comprising an irreversible gastric H+ / K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor, pentagastrin (PG) or a PG analogue as an activator of parietal cells in the gastric lumen. In a preferred embodiment, the composition further comprises at least one agent that preserves the availability of PG in the gastric fluids, thus enabling PG to act locally in the stomach. Unexpectedly, the compositions of the present invention exhibit anti-acid activity locally in the stomach that is meal-independent, exhibit fast onset and prolonged inhibition of acid secretion.

An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and / or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage form in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.

The present invention relates to a class of new tetrahydrocyclopenta[c]pyrrole derivatives represented by a general formula (I) and a preparation method thereof, a pharmaceutical composition containing the derivative, and uses of the tetrahydrocyclopenta[c]pyrrole derivative as the treatment agent, particularly the gastric acid secretion inhibitor and the potassium ion competitive acid blocker (P-CABs). Each substituent in the general formula (I) is defined in the specification. The general formula (I) is defined in the specification.

The present invention relates to the use of pharmaceutically acceptable zinc salts, preferably water soluble zinc salts alone or optionally, in combination with one or more of a protein pump inhibitor (PPI), H2 blocker, anti-H. pylori antibiotic / antimicrobial, cytoprotective agent or a combination agent as otherwise described herein for providing fast action with optional long duration effect in reducing gastric acid secretion, raising the pH of the stomach during resting phase as well as decreasing the duration of stomach acid release during a secretagogue phase and for treating conditions including gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), Zollinger-Ellison syndrome (ZE disease), ulcer disease, and gastric cancer, as well as preventing or reducing the likelihood of ulcer disease. In addition, the present methods are useful for treating patients who are non-responsive to proton pump inhibitors (PPI) and as an alternative to traditional therapies or conditions which are caused by rapid and complete inhibition of secretagogue induced acid secretion. The present invention also relates to the use of one or more water soluble zinc salts, administered in combination with a therapeutic compound or agent (second therapeutic agent) which may be delivered orally with enhanced bioavailability (compared to compounds which are administered in the absence of water soluble zinc salts) or other favorable benefits. In addition, therapeutic agents which exhibit sensitivity to low pH may be advantageously orally administered in combination with an effective amount of at least one water soluble zinc salt. Compositions according to the present invention exhibit greater bioavailability of the active agent when formulated in combination with a water soluble zinc salt in oral dosage form than when administered with the water soluble zinc salt.

The present invention relates to the use of pharmaceutically acceptable zinc salts, preferably water soluble zinc salts alone or optionally, in combination with one or more of a protein pump inhibitor (PPI), H2 blocker, anti-H. pylori antibiotic / antimicrobial, cytoprotective agent or a combination agent as otherwise described herein for providing fast action with optional long duration effect in reducing gastric acid secretion, raising the pH of the stomach during resting phase as well as decreasing the duration of stomach acid release during a secretagogue phase and for treating conditions including gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), Zollinger-Ellison syndrome (ZE disease), ulcer disease, and gastric cancer, as well as preventing or reducing the likelihood of ulcer disease. In addition, the present methods are useful for treating patients who are non-responsive to proton pump inhibitors (PPI) and as an alternative to traditional therapies or conditions which are caused by rapid and complete inhibition of secretagogue induced acid secretion.

An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety.The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric / duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.

The present invention is related to novel oral compositions comprising an irreversible gastric H+ / K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more aliphatic carboxylic acid derivative molecules which activate parietal cells, wherein the derivatives possess delayed or sustained enhancement effect on the PPI activity compared to the non-derivatized acid molecules. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.

The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same.Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula:(wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.

The present invention is directed to compositions having an effective amount of Adenosine Triphosphate (“ATP”) sufficient to effect intracellular and extracellular concentrations of ATP in a mammal to improve anaerobic exercise capacity by increasing muscle size and / or strength and methods for using the same. Preferably, a gastric acid secretion inhibitory coating is applied to the effective amount of ATP in a manner that protects the ATP from degradation by gastric juices. ATP compositions of the present invention may be administered in nutraceutical or functional food dosage forms, including oral and non-oral delivery forms. In addition, the effective amount of ATP maybe combined with amino acids, botanicals, functional foods, herbals, nucleotides, nutraceuticals, nutrients, pharmaceuticals, proteins, and / or vitamins in an effort to enhance the targeted activity of the composition.

The present invention provides a crystalline form of a 5-(2-fluorophenyl)-N-methyl-1-(3-pyridylsulfonyl)-1H-pyrrole-3-methylamine salt compound, the crystalline form is characterized in that in an X-ray powder diffraction spectrum obtained by Cu-K [alpha] radiation and represented by 2 [theta] angle, the crystalline form of the 5-(2-fluorophenyl)-N-methyl-1-(3-pyridylsulfonyl)-1H-pyrrole-3-methylamine salt compound has characteristic diffraction peaks at 9.7, 10.1, 15.2, 17.8, 20.3, 24.9 and 25.8. The crystalline form has good stability and solubility. A preparation method of the crystalline form is also provided.

An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and / or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage form in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.

Systems and methods for delivering oral administration of ATP in a manner that protects the ATP from degradation by gastric juices through enteric coating to enhance absorption into the blood stream and provide additional therapeutic benefit when compared with non-protected forms of ATP. Said systems and methods comprising a composition used for improving muscle torque and reducing muscle fatigue, said composition comprising an effective amount of ATP. Preferably, a gastric acid secretion inhibitory coating is applied to the effective amount of ATP in a manner that protects the ATP from degradation by gastric juices. Said systems and methods effecting intracellular and extracellular ATP concentrations and increasing human performance by reducing muscle fatigue and recovery time which comprises administering an effective amount of ATP to a human. Alternatively, an effective amount of ATP may be administered sublingually, thereby avoiding exposure to gastric juices. The effective amount of ATP may be delivered by means of a tablet, granules, microgranules or powders.

An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.

The invention belongs to the technical field of medicines, and concretely relates to a rabeprazole sodium hydrate and its preparation method. The rabeprazole sodium hydrate obtained in the invention contains one crystal water, has a good stability, and has an unobvious moisture absorption weight increment under highly humid conditions, and the gastric acid secretion inhibition effect of the hydrate is 20% higher than that of a rabeprazole sodium tablet. The invention also relates to applications of compositions of the hydrate in the treatment of digestive system diseases comprising duodenal ulcer, gastric ulcer, reflux esophagitis and the like.

A pyrrolopyridazine compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. (In the formula, R<1> is C2-6 alkenyl, C2-6 halogenoalkenyl, optionally substituted C3-7 cycloalkyl, or optionally substituted C1-6 alkyl substituted by C3-7 cycloalkyl; R<2> is C1-6 alkyl; R<3> is hydroxymethyl, C2-6 aliphatic acyloxymethyl, optionally substituted (C6-10 aryl)carbonyloxymethyl, (C1-6 alkoxy)carbonyloxymethyl, formyl, carboxy, (C1-6 alkoxy)carbonyl, or optionally substituted (C6-10 aryl)oxycarbonyl; R<4> is optionally substituted C6-10 aryl; and A is imino, oxygen, or sulfur.) The pyrrolopyridazine compound is highly effective in inhibiting the secretion of gastric hydrochloric acid, protecting the gastric mucosa, and the like. It is useful as a medicine, especially a preventive / remedy for ulcerative diseases.

It is an object of the present invention to provide (1) a process for manufacturing alkali metal salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole which are useful as gastric acid secretion inhibitors, anti-ulcer agents and other drugs and (2) salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole with amines which are intermediates for the production of the alkali metal salts, and a process for manufacturing the same. According to the present invention, disclosed are salts represented by the following formula (I): (wherein A+ represents an isopropylammonium ion, sec-butylammonium ion or cyclopentylammonium ion).

A pharmaceutical composition for use in oral medication for the treatment of diabetes mellitus can include an antacid agent with an enteric coating, which permits the antacid agent to be delivered in the small intestine where it reduces acidity thereby causing a lowering of blood sugar levels. The pharmaceutical composition can be packaged in various tablet forms, including standard tablets and multiple pellet tablets. The pharmaceutical composition can further include a composition for treatment of diabetes, such as metformin, in enteric or non-enteric formulations. The pharmaceutical composition can further include an enteric-coated gastric acid secretion inhibitor. Also disclosed are methods for the treatment of diabetes mellitus, using the pharmaceutical composition and its variants.

The invention belongs to the technical field of medicine, and particularly relates to a rabeprazole sodium sesquihydrate and a preparation method thereof. The rabeprazole sodium sesquihydrate prepared by the invention contains a hemicrystalline water, and has the advantages that the rabeprazole sodium sesquihydrate is high in purity and stability, and the phenomena of weight increasing due to moisture absorption even under a high-humidity condition are not obvious; the gastric acid secretion inhibition effect of the rabeprazole sodium sesquihydrate is improved by about 20 percent. The invention further relates to application of a composition comprising the sesquihydrate to treat digestive system diseases such as duodenal ulcers, gastric ulcers and reflux esophagitis.

Disclosed herein are kits useful for facilitating compliance with a treatment regimen. In one embodiment, the kits are useful for compliance with a defined method of treatment which utilizes a composition comprising a gastric acid secretion inhibitor. In an alternative or additional embodiment, the kits comprise an outer container and at least two inner containers, wherein each of the inner containers comprise, independently, a plurality of unit doses of a composition comprising a therapeutically effective amount of a gastric acid secretion inhibitor.

The invention relates to a novel application of a gastric acid secretion inhibitor. The novel application is that vonoprazan fumarate is injected into human body through intravenous administration to inhibit gastric acid secretion, the pH value of stomach is increased, at the same time, the activity of pepsin is inhibited, on the other aspect, the factor of damaging mucosa is reduced, blood platelets can aggregate on the bleeding parts more easily, the solidified blood clots are difficult to dissolve, the blood can be stopped in the bleeding parts, the blood solidification is promoted, the blood crust is stabilized, and the mucosa is repaired. The gastric acid secretion inhibitor can be used to treat and prevent subsequent acute damage of gastric mucosa under a stress state, severe diseases (cerebral hemorrhage, severe wounds, etc.), and upper gastrointestinal hemorrhage caused by gastric operation.

The present invention is related to novel oral compositions comprising an irreversible gastric H+ / K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, 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.