Composition and method for treatment of diabetes
Inventors
Assignees
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Publication Number
US-8680085-B2
Publication Date
2014-03-25
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 conditions of an individual by stimulating gut hormone secretion from L-cells in the colon. It specifies one or more incretin-related metabolic conditions including type I diabetes, type II diabetes, hypertriglyceridemia, obesity, appetite control, metabolic syndrome, and polycystic ovary syndrome. The approach uses a composition selected to cause gut hormone secretion from L-cells.
The stimulating pharmaceutical composition causes release of gut hormones from L-cells in the colon, including GLP-1, GLP-2, PYY, and oxyntomodulin. The composition is selected from the group comprising bile acid and salts thereof, and is delivered via a colon targeted delivery system configured as a controlled release formulation. The document describes bypassing the upper digestive tract to achieve colon release and L-cell stimulation.
The colon targeted delivery system is described as a matrix within matrix system implemented as a multimatrix “matrix-in-matrix” controlled/targeted delivery system. The formulation includes a hydrophilic first matrix and a dispersed second matrix with lipophilic and amphiphilic phases. The active agent is described as distributed in the amphiphilic phase within the second matrix, within the hydrophilic first matrix.
Claims Coverage
The partial content identifies one independent claim (clm-00001) and a dependent claim (clm-00002) that further defines the colon-targeted delivery system. The independent claim includes inventive features centered on selecting a bile acid or salt composition that causes L-cell gut hormone secretion, formulating it in a colon-targeted controlled release matrix-in-matrix system, and administering a sufficient amount to trigger gut hormone release in the colon to achieve a desired result.
Bile acid selection for L-cell gut hormone secretion
Selecting a composition causing gut hormone secretion from L-cells from the group comprising a bile acid and salts thereof.
Colon-targeted controlled release matrix-in-matrix formulation
Formulating the composition as a controlled release formulation formulated to release in a colon targeted delivery system comprising a matrix within matrix system.
Administering sufficient composition to trigger colon release of gut hormones
Administering sufficient stimulating pharmaceutical composition to the individual sufficient to cause a release of gut hormones from the L-cell in the colon of the individual sufficient to achieve the desired result.
Hydrophilic first matrix with dispersed second matrix including amphiphilic phase
Wherein the colon targeted delivery system is a controlled release formulation of a hydrophilic first matrix comprising a lipophilic phase and an amphiphilic phase in a second matrix dispersed throughout the hydrophilic first matrix, with the agent at least partially incorporated into the amphiphilic phase.
Across the independent and dependent claims, the core claim coverage centers on bile acid or salt compositions that cause gut hormone secretion from L-cells in the colon, delivered via a colon-targeted controlled release matrix-within-matrix system, with the dependent claim specifying a hydrophilic first matrix and a dispersed second matrix having amphiphilic phase incorporation of the agent.
Stated Advantages
Achieves desired therapeutic result by causing release of gut hormones from L-cells in the colon.
Treats one or more specified conditions including type I diabetes, type II diabetes, hypertriglyceridemia, obesity, appetite control, metabolic syndrome, and polycystic ovary syndrome.
Documented Applications
Treating type I diabetes, type II diabetes, hypertriglyceridemia, obesity, appetite control, metabolic syndrome, and polycystic ovary syndrome by colon-targeted delivery to stimulate L-cell gut hormone release.
Rectal release system dosing with glutamine/butyric acid with reported measurements of GLP-1/PYY and reported metabolic outcomes using HbA1c, fasting glucose, and OGTT endpoints.
MMX tablet dosing of glutamine/butyric acid with reported decreased glucose outcomes over a multi-week regimen and measurement using HbA1c/fasting glucose/OGTT endpoints.
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