Composition and method for treatment of diabetes
Inventors
Assignees
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Publication Number
US-8470885-B2
Publication Date
2013-06-25
Expiration Date
Abstract
The present invention relates to a method of treating an incretin related disease such as diabetes, obesity and the like by delivery of butyric acid, bile acid, long chain fatty acid, or glutamine to the colon by bypassing the upper digestive tract.
Core Innovation
The invention relates to treating incretin-related metabolic diseases by stimulating the production and release of a gut hormone secreted from L-cells in the colon. The biological rationale stated is that L-cells in the colon secrete GLP-1, GLP-2, PYY, and oxyntomodulin. The disclosed approach targets conditions associated with a decrease or lack of release of an L-cell secreted gut hormone.
The disclosed problem is a decrease or lack of release of a gut hormone secreted from L-cells, which is described as affecting type I diabetes, type II diabetes, obesity, appetite control, metabolic syndrome, polycystic ovary syndrome, and hypertriglyceridemia. The solution proposed is to stimulate L-cell gut hormone production in the colon by administering gut-hormone-stimulation agents formulated to act in the colon.
The invention uses compositions selected from butyric acid and glutamine that are formulated for colon targeted delivery or for a rectal release system. The delivery system bypasses the stomach and upper GI tract by not releasing in the stomach or upper gastro intestinal tract, while enabling release in the colon. In further embodiments, the colon-targeted delivery system is a controlled-release matrix-within-matrix formulation having a hydrophilic first matrix and a second matrix formed by lipophilic and amphiphilic phases, with the active incorporated at least partially in the amphiphilic phase.
Claims Coverage
The partial claims provided include two independent claims covering a method of treating listed incretin-related metabolic conditions by colon or rectal stimulation of L-cells to release a gut hormone, and a composition for inducing release of a gut hormone from colon L-cells that does not release in the stomach or upper GI tract. Across the independent claims, the inventive features include selecting butyric acid and/or glutamine, colon-targeted or rectal formulation, and, in narrower coverage, matrix-within-matrix controlled-release structure specifying hydrophilic first matrix and dispersed second matrix formed by lipophilic and amphiphilic phases.
Colon and rectal stimulation of L-cells for gut hormone release
A method treating type I diabetes, type II diabetes, hypertriglyceridemia, obesity, appetite control, metabolic syndrome, or polycystic ovary syndrome affected by the decrease or lack of release of a gut hormone secreted from L-cells by stimulating the production of an L-cell secreted gut hormone in the colon of an individual.
Selecting butyric acid and glutamine for colon/rectal release
Selecting a composition causing gut hormone secretion from L-cells from the group comprising butyric acid and glutamine, wherein the composition is formulated to release in a colon targeted delivery system or in a rectal release system.
Administering to colon or rectum to achieve desired gut hormone release
Administering sufficient stimulating pharmaceutical composition to the individual colon or rectum sufficient to cause a release of gut hormones from the L-cell in the colon of the individual sufficient to achieve the desired result.
Composition that induces colon L-cell gut hormone release without stomach/upper GI release
A composition for inducing the release of a gut hormone from L-cells in the colon, wherein the composition comprises a composition selected from the group comprising butyric acid and glutamine formulated such that it does not release in either the stomach or upper gastro intestinal tract.
Colon targeted delivery system or rectal formulation for the composition
Formulating the butyric acid and/or glutamine composition in a colon targeted drug delivery system or formulated for rectal administration.
Matrix-within-matrix controlled-release structure with hydrophilic first matrix and amphiphilic-phase incorporation
A controlled-release formulation for the colon targeted delivery system comprising a hydrophilic first matrix and a second matrix dispersed throughout the hydrophilic first matrix, wherein the second matrix is formed by lipophilic and amphiphilic phases and the composition is at least partially incorporated into the amphiphilic phase.
Overall claim coverage is directed to stimulating L-cells in the colon to release a gut hormone, using compositions selected from butyric acid and glutamine, delivered so that release occurs in the colon via colon-targeted delivery or rectal release and does not release in the stomach or upper GI tract. In narrower embodiments, the colon-targeted controlled-release formulation is defined as a matrix-within-matrix structure with a hydrophilic first matrix and a dispersed second matrix formed by lipophilic and amphiphilic phases, with the active incorporated at least partially into the amphiphilic phase.
Stated Advantages
Stimulates L-cell gut hormone production and release in the colon.
Targets release in the colon while not releasing in the stomach or upper gastro intestinal tract.
Uses a colon-targeted controlled-release matrix-within-matrix formulation including hydrophilic first matrix and dispersed second matrix formed by lipophilic and amphiphilic phases.
Documented Applications
Treating type I diabetes, type II diabetes, hypertriglyceridemia, obesity, appetite control, metabolic syndrome, or polycystic ovary syndrome affected by a decrease or lack of release of an L-cell secreted gut hormone.
Inducing the release of a gut hormone from L-cells in the colon using a composition comprising butyric acid and/or glutamine formulated to avoid release in the stomach and upper gastro intestinal tract.
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