Chemosensory receptor ligand-based therapies
Inventors
Baron, Alain D. • Beeley, Nigel R. A. • Fineman, Mark S.
Assignees
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Publication Number
US-10610500-B2
Publication Date
2020-04-07
Expiration Date
Abstract
Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
Core Innovation
The invention relates to a method of lowering blood glucose levels in a subject in need thereof by administering a composition comprising metformin or a salt thereof. The composition is adapted for delivery to enteroendocrine cells distal of the duodenum and provides a lower average bioavailability of metformin as compared to an immediate-release formulation of an equivalent amount of metformin.
The disclosed approach further relates to controlling the onset of release of orally administered bitter receptor ligand compositions in a time-dependent manner and in a pH-dependent manner. The compositions are adapted to release a therapeutically effective amount of the bitter receptor ligand to one or more regions of the intestine, including downstream of the duodenum, downstream of the jejunum, the ileum, lower intestine, and other stated intestinal segments.
The disclosure also provides bitter receptor ligand excipients and multiple classes of bitter taste receptor ligands defined by structural Formulae and variable substituents, including plant extract options, natural products, and representative example chemical structures. The ligands are framed as bitter receptor ligand and taste receptor ligand within the scope of the disclosed embodiments.
Claims Coverage
The provided claim set identifies one independent claim focused on lowering blood glucose by metformin administration with distal intestinal delivery and reduced average bioavailability relative to an immediate-release formulation. The claim coverage also includes bitter receptor ligand compositions adapted for intestinal release to one or more regions of the intestine.
Metformin distal enteroendocrine-cell delivery with lower average bioavailability
A method of lowering blood glucose levels in a subject in need thereof by administering a composition comprising metformin or a salt thereof, wherein the composition is adapted for delivery to enteroendocrine cells distal of the duodenum and provides a lower average bioavailability of metformin as compared to an immediate-release formulation of an equivalent amount of metformin.
Bitter receptor ligand release to intestinal regions
A composition adapted to release a therapeutically effective amount of a bitter receptor ligand to one or more regions of the intestine.
pH-dependent onset of release
The composition provides an onset of release at about pH 6.0, about pH 6.5, about pH 7.0, or a combination thereof.
Across the provided claim information, the central inventive concepts are distal enteroendocrine delivery of metformin with lower average bioavailability than immediate release, together with bitter receptor ligand compositions adapted for intestinal release and pH-dependent onset behavior.
Stated Advantages
Lowers blood glucose levels in a subject in need thereof.
Provides a lower average bioavailability of metformin as compared to an immediate-release formulation of an equivalent amount of metformin.
Minimize metformin plasma absorption and reducing average bioavailability while still achieving enteroendocrine activation.
Documented Applications
A method of lowering blood glucose levels in a subject in need thereof using a metformin or salt composition adapted for delivery to enteroendocrine cells distal of the duodenum.
Intestinal delivery of bitter receptor ligand excipients to one or more regions of the intestine with release of a therapeutically effective amount of the bitter receptor ligand.
Use of bitter taste receptor ligand classes in other embodiments as taste receptor ligand material with variable substitutions and representative example chemical structures.
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