Colon-Targeted Glutamine Delivery for Diabetes Treatment
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Solution Overview
Problem
Current treatments for Type II diabetes, obesity, and related conditions face challenges due to the difficulty in administering and stabilizing gut hormones like GLP-1, which are essential for regulating blood glucose levels, as they are unstable and unpalatable, making it hard to deliver them effectively to the colon for pharmacological action.
Innovation Solution
A composition comprising glutamine, formulated in a colon-targeted drug delivery system that bypasses the stomach and upper digestive system, using methods such as covalent linkage, polymer coatings, or matrix-within-matrix systems to stimulate the release of gut hormones like GLP-1, GLP-2, and oxyntomodulin from L-cells in the colon, thereby addressing the lack of hormone secretion associated with these conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If gut hormones like GLP-1 are administered to treat diabetes, then insulin secretion and glucose regulation are improved, but the hormones are unstable and degrade in the digestive tract, making effective delivery difficult
Solution Approach 1:
The patent uses an intermediary substance (glutamine or its derivatives) that is stable in the digestive tract but can be converted to the active gut hormone GLP-1 in the colon. This intermediary acts as a precursor that bypasses the stability issue of direct GLP-1 administration while still achieving the desired therapeutic effect through endogenous hormone production.
Solution Approach 2:
The invention extracts the essential therapeutic function (stimulating GLP-1 production) from the unstable hormone itself. Instead of administering the unstable GLP-1 directly, the patent removes the problematic hormone and replaces it with a stable precursor substance that can be converted to the active hormone at the target site, thereby separating the delivery vehicle from the active agent.
2Reliability
If GLP-1 is administered to stimulate insulin secretion, then diabetes treatment effectiveness is improved, but the peptide is unpalatable and difficult to administer
Solution Approach 1:
The patent employs a disposable precursor substance (glutamine) that is stable, palatable, and easy to administer orally. This precursor is converted to the active hormone in the body, eliminating the need for complex administration procedures required for direct peptide delivery. The solution replaces a difficult-to-administer active agent with an easy-to-administer precursor.
Solution Approach 2:
Instead of administering the original unstable and unpalatable GLP-1 peptide, the patent uses a stable precursor (glutamine) that copies or mimics the ultimate therapeutic effect by being converted to GLP-1 in the colon. This creates a functional copy of the therapeutic action without the drawbacks of the original molecule.
3Reliability
If glutamine is delivered orally to stimulate GLP-1 production, then hormone secretion is improved, but glutamine degrades in the stomach and upper digestive system
Solution Approach 1:
The patent modifies the delivery system to provide different properties at different locations in the digestive tract. The formulation is designed to resist degradation in the stomach and upper intestine while releasing glutamine specifically in the colon where L-cells are present. This local targeting ensures the substance reaches its destination intact while performing its function only where needed.
Solution Approach 2:
The digestive tract delivery system is segmented into different zones with different release characteristics. The formulation is designed to pass through the stomach and upper intestine without degrading or releasing the active ingredient, then release glutamine specifically in the colon. This segmentation allows the substance to avoid degradation zones while targeting the therapeutic zone.
Data Source
AI summary
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.