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Novel substituted benzimidazole dosage forms and method of using same

a technology of benzimidazole and dosage forms, which is applied in the direction of drug compositions, inorganic non-active ingredients, dispersed delivery, etc., can solve the problems of negation of benefits

Inactive Publication Date: 2005-01-06
UNIVERSITY OF MISSOURI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to pharmaceutical preparations containing substituted benzimidazole proton pump inhibitors, specifically omeprazole, lansoprazole, and other proton pump inhibitors. These drugs are commonly used to treat conditions such as duodenal ulcers, gastric ulcers, gastroesophageal reflux disease, and peptic ulcers. However, they have certain disadvantages such as not being completely effective and producing adverse side effects. The invention aims to provide a new formulation that can minimize the pain and complications associated with these conditions. The technical effect of the invention is to provide a more effective and safe treatment for stress-related gastric mucosal damage and upper gastrointestinal bleeding, which is a common problem in critically ill patients.

Problems solved by technology

Although micronization results in increased surface area possibly causing particle aggregation, which can negate the benefit of micronization and is an expensive manufacturing step, it does have the significant benefit of increasing the dissolution rate of relatively water insoluble drugs, such as omeprazole and other proton pump inhibiting agents.
When added to water the acids and base react to liberate carbon dioxide, resulting in effervescence.

Method used

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  • Novel substituted benzimidazole dosage forms and method of using same
  • Novel substituted benzimidazole dosage forms and method of using same
  • Novel substituted benzimidazole dosage forms and method of using same

Examples

Experimental program
Comparison scheme
Effect test

example i

A. Fast Disintegrating Suspension Tablets of Omeprazole.

A fast disintegrating tablet is compounded as follows: Croscarmellose sodium 300 g is added to the vortex of a rapidly stirred beaker containing 3.0 kg of deionized water. This slurry is mixed for 10 minutes. Omeprazole 90 g (powdered) is placed in the bowl of a Hobart mixer. After mixing, the slurry of croscarmellose sodium is added slowly to the omeprazole in the mixer bowl, forming a granulation, which is then placed in trays and dried at 70° C. for three hours. The dry granulation is then placed in a blender, and to it is added 1,500 g of Avicel® AC-815 (85% microcrystalline cellulose coprocessed with 15% of a calcium, sodium alginate complex) and 1,500 g of Avicel® PH-302 (microcrystalline cellulose). After this mixture is thoroughly blended, 35 g of magnesium stearate is added and mixed for 5 minutes. The resulting mixture is compressed into tablets on a standard tablet press (Hata HS). These tablets have an average we...

example ii

Standard Tablet of Proton Pump Inhibitor and Buffering Agent.

Ten (10) tablets were prepared using a standard tablet press, each tablet comprising about 20 mg omeprazole and about 975 mg sodium bicarbonate uniformly dispersed throughout the tablet. To test the disintegration rate of the tablets, each was added to 60 ml of water. Using previously prepared liquid omeprazole / sodium bicarbonate solution as a visual comparator, it was observed that each tablet was completely dispersed in under three (3) minutes.

Another study using the tablets compounded according to this Example evaluated the bioactivity of the tablets in five (5) adult critical care subjects. Each subject was administered one tablet via ng with a small amount of water, and the pH of ng aspirate was monitored using paper measure. The pH for each subject was evaluated for 6 hours and remained above 4, thus demonstrating the therapeutic benefit of the tablets in these patients.

Tablets were also prepared by boring out...

example iii

Proton Pump Inhibitor Central Core Tablet.

Tablets are prepared in a two-step process. First, about 20 mg of omeprazole is formed into a tablet as is known in the art to be used as a central core. Second, about 975 mg sodium bicarbonate USP is used to uniformly surround the central core to form an outer protective cover of sodium bicarbonate. The central core and outer cover are both prepared using standard binders and other excipients to create a finished, pharmaceutically acceptable tablet. The tablets may be swallowed whole with a glass of water.

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Abstract

Disclosed herein are methods, kits, combinations, and compositions for treating gastric acid disorders employing pharmaceutical compositions comprising a proton pump inhibiting agent (PPI) and a buffering agent in a pharmaceutically acceptable carrier.

Description

TECHNICAL FIELD The present invention relates to pharmaceutical preparations comprising substituted benzimidazole proton pump inhibiting agents. BACKGROUND OF THE INVENTION Omeprazole is a substituted benzimidazole, 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl) methyl]sulfinyl]-1H-benzimidazole, that inhibits gastric acid secretion. Omeprazole belongs to a class of antisecretory compounds called proton pump inhibitors proton pump inhibiting agents (“PPIs”) that do not exhibit anti-cholinergic or H2 histamine antagonist properties. Drugs of this class suppress gastric acid secretion by the specific inhibition of the H+. K+-ATPase enzyme system (proton pump) at the secretory surface of the gastric parietal cell. Typically, omeprazole, lansoprazole and other proton pump inhibitors are formulated in an enteric-coated solid dosage form (as either a delayed-release capsule or tablet) or as an intravenous solution (as a product for reconstitution), and are prescribed for short-term ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/10A61K9/00A61K9/14A61K9/20A61K9/22A61K9/24A61K9/28A61K9/46A61K9/48A61K31/00A61K31/4439A61K33/00A61K36/185A61K36/42A61K36/48A61K36/534A61K36/898A61K45/06A61K47/02A61K47/04A61K47/12A61K47/24A61P1/04A61P1/06A61P43/00
CPCA61K9/0007A61K9/0056A61K47/02A61K45/06A61K36/898A61K36/534A61K36/48A61K36/42A61K36/185A61K33/00A61K31/4439A61K31/00A61K9/2813A61K9/209A61K9/2086A61K9/0095A61K9/2009A61K9/2013A61K9/2054A61K9/2081A61K2300/00A61P1/00A61P1/04A61P1/06A61P43/00A61K31/4184
Inventor PHILLIPS, JEFFREY O.
Owner UNIVERSITY OF MISSOURI
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