Compositions comprising bile acid sequestrants for treating esophageal disorders
Inventors
Assignees
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Publication Number
US-9205094-B2
Publication Date
2015-12-08
Expiration Date
Abstract
Compositions comprising a therapeutically effective amount of at least one bile acid sequestrant are disclosed for treating or preventing upper GI tract disorders and protecting stratified squamous epithelium against injury by a noxious substance. Exemplary bile acid sequestrants include colesevelam, colesevelam hydrochloride, colestipol, sevelamer and combinations thereof. The disclosed methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising at least one bile acid sequestrant, alone or in combination with at least one proton pump inhibitor.
Core Innovation
The invention relates to a sustained-release pharmaceutical dosage form for oral administration to a subject in need thereof that comprises an amount of at least one bile acid sequestrant in a range from 0.1 g to 1.0 g. The bile acid sequestrant is selected from colesevelam, colesevelam hydrochloride, colestipol, sevelamer, and combinations thereof, and the dosage form further comprises a gastric-retention vehicle composition comprising one or more hydrogels.
The gastric-retention vehicle composition is defined such that the dosage form expands upon contact with gastric fluid. The sustained-release dosage form uses the hydrogel-based gastric-retention vehicle to maintain the dosage form in the stomach by expanding when exposed to gastric fluid.
Additional disclosed embodiments optionally include a proton pump inhibitor in a therapeutically effective amount. The disclosed proton pump inhibitor options include omeprazole and other proton pump inhibitors, and the document also references formulation variants including adding antacids or histamine H2-receptor antagonists and kit formats comprising the bile acid sequestrant and optionally the proton pump inhibitor.
Claims Coverage
The independent claims center on a sustained-release oral dosage form that combines a specified bile acid sequestrant amount with a gastric-retention hydrogel vehicle that expands in gastric fluid. Dependent claim refinements add a proton pump inhibitor and further narrow gastric retention and formulation proportions.
Sustained-release oral dosage form with expanding gastric-retention hydrogel
A sustained-release pharmaceutical dosage form for oral administration comprising an amount of at least one bile acid sequestrant in a range from 0.1 g to 1.0 g, wherein the bile acid sequestrant is selected from colesevelam, colesevelam hydrochloride, colestipol, sevelamer, and combinations thereof, and a gastric-retention vehicle composition comprising one or more hydrogels, wherein the dosage form expands upon contact with gastric fluid.
Therapeutically effective proton pump inhibitor amount
A sustained-release pharmaceutical oral dosage form further includes a therapeutically effective amount of at least one proton pump inhibitor in a range from 1 mg to 200 mg.
Gastric retention for three hours or more
The sustained-release oral pharmaceutical dosage form is retained in a person's stomach for three hours or more after ingestion.
Active ingredient proportion of total weight
Active ingredient(s) make up about 10% to about 75% of the total weight.
Overall, the claim coverage centers on an oral sustained-release dosage form that expands in gastric fluid via a hydrogel gastric-retention vehicle and includes a bile acid sequestrant amount within 0.1 g to 1.0 g. Dependent claim refinements cover adding a therapeutically effective proton pump inhibitor amount and further narrowing gastric retention and formulation proportions.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Example studies assessing effects on esophageal epithelial cells and rodent Barrett’s esophagus models.
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