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Publication Number

US-11564910-B2

Patent

Publication Date

2023-01-31

Expiration Date


Abstract

Described herein are pharmaceutical compositions including omeprazole and a benzimidazole drug. In some embodiments, the compositions can be formulated for oral administration. The compositions can be used to treat gastrointestinal conditions. Methods of treatment using the compositions are also described.

Core Innovation

The invention relates to pharmaceutical compositions for treating or preventing gastrointestinal conditions, with an emphasis on gastrointestinal ulcers. The compositions combine a proton pump inhibitor, including omeprazole, with a benzimidazole antiparasitic drug, including named benzimidazole members such as fenbendazole and carbendazim.

The disclosed compositions are positioned to provide a surprising synergistic and/or additive drug effect when compared with omeprazole alone. The described effect includes faster ulcer recovery and reduced drug burden and reduced side effects. The disclosure reports treatment outcomes in horses and camels using the claimed combination approach and includes ulcer grading improvements after a number of days to weeks.

The disclosure further defines benzimidazole chemical structures using a formula (I) with structural variables and ranges, and it lists benzimidazole member compounds. Formulation options include oral liquid, paste, and non-solid formulations, and optional excipients are described, including polyethylene glycol, carboxymethyl cellulose, sodium sulfite, and sodium bicarbonate.

Claims Coverage

The independent claim coverage is centered on a single composition claim, defining a proton pump inhibitor in combination with a compound of a specified formula, or a pharmaceutically acceptable salt. The main inventive features include two features.

Proton pump inhibitor combined with a formula-defined heterocyclic compound

A composition comprising a proton pump inhibitor and a compound having the formula, or a pharmaceutically acceptable salt thereof, with X1–X23, R1–R9, and indices n, m, p, and r defining the allowable structure variables and ranges for the compound.

Structural variable ranges defining acceptable compound embodiments

The compound component is defined such that various substituent-position variables X1–X23 and bond/option variables X13–X23 are each limited to specified choices, and R1, R2, R3, R4, R5, R6, R7, R8, R9, and the indices n, m, p, and r are each constrained to listed alternatives and ranges.

Across the independent claim, the inventive scope is defined by the combination of a proton pump inhibitor with a compound characterized by a structured formula, including pharmaceutically acceptable salts, and by constraints on the compound’s structural variables and indices.

Stated Advantages

Faster ulcer recovery compared with omeprazole alone.

Reduced drug burden versus omeprazole alone.

Reduced side effects versus omeprazole alone.

Documented Applications

Treatment of gastrointestinal conditions, including gastrointestinal ulcers, by administering the claimed composition to a mammal, as described for horses and camels in the disclosure.

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