Delayed Release Hops Extract Capsule for Appetite Control
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Solution Overview
Problem
Existing weight management products are often ineffective and come with unpleasant side effects, and hops extracts, particularly iso-acids, have limitations in activating bitter taste receptors and may be off-putting due to bitterness.
Innovation Solution
A delayed release oral dosage form comprising a hops extract with a high alpha acid content, specifically cohumulone, which is not isomerised, to effectively bind to TAS2R40 and TAS2R14 in the gastrointestinal tract, thereby modifying energy intake and appetite.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If hops extracts are prepared in powder form to avoid nausea and side effects, then tolerability is improved, but weight management effectiveness is reduced due to lack of TAS2R40 activation
Solution Approach 1:
The patent changes the physical state parameter from powder to liquid/capsule form, and modifies the chemical composition by using native acids instead of isomerised acids. This allows the extract to activate TAS2R40 receptors in the gastrointestinal tract while maintaining tolerability through delayed release formulation that prevents nausea.
2Ease of operation
If iso-acids are used in hops extracts, then bitterness is increased which may be off-putting to consumers, but the patent aims to maintain bitterness for TAS2R activation
Solution Approach 1:
The patent applies local quality by distinguishing between oral bitterness (TAS2R1) and gastrointestinal bitterness (TAS2R40). The native acids provide necessary bitterness for TAS2R40 activation in the GI tract while the delayed release formulation prevents excessive oral bitterness from causing consumer rejection.
3Reliability
If caffeine is used in weight loss products to suppress appetite, then appetite suppression is achieved, but tolerance develops over time and side effects occur
Solution Approach 1:
The patent substitutes the mechanical/chemical stimulation mechanism of caffeine with a receptor-based mechanism involving TAS2R40 activation by native hops acids. This biological pathway does not induce tolerance in the same way caffeine does, providing sustained effectiveness without the tolerance problem.
4Object-affected harmful factors
If delayed release formulation is used, then tolerability is improved by avoiding nausea, but the complexity of the dosage form increases
Solution Approach 1:
The patent uses a delayed release capsule as an intermediary delivery system. This intermediary formulation modifies the release profile of the native hops acid extract, allowing it to bypass the stomach and release in the intestine where it activates TAS2R40 receptors without causing nausea.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The oral dosage form reduces energy intake, modifies subjective ratings of appetite, and increases gut peptide hormone concentrations, providing an effective and tolerable means for weight management.
Implementation Method 1
activation of specific bitter taste receptors (TAS2Rs), expressed throughout the gastrointestinal (GI) tract by enteroendocrine cells, can modulate feeding behaviour via release of gut peptide hormones
Data Source
AI summary
This invention provides novel oral dosage forms comprising a hops extract. The oral dosage forms are capable of activating bitter taste receptors expressed in the gastrointestinal tract. The applications include but are not limited to the use of the oral dosage forms for reducing energy intake and/or appetite in a subject.