Meltable Tablet Formulation Bypassing Liver First-Pass Metabolism
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Solution Overview
Problem
Existing active ingredients like berberine, spermidine, and others are scarce and expensive, making them difficult to use in large quantities for everyday applications, and their efficacy is hindered by liver metabolism during oral administration.
Innovation Solution
A meltable tablet formulation containing disaccharides and phosphatidylcholine, such as trehalose and sunflower lecithin, allows direct absorption through the oral mucosa, bypassing liver metabolism and enhancing therapeutic potential.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If active ingredients are administered orally in conventional form, then they are delivered to the human organism, but they undergo liver metabolism (first-pass effect) which reduces their efficacy
Solution Approach 1:
The patent uses oral mucosa as an intermediary absorption route between the administered active ingredient and the bloodstream. The mucoadhesive tablet formulation enables the active ingredient to be absorbed directly through the oral mucosa, bypassing the liver's first-pass metabolism and thereby maintaining therapeutic efficacy while reducing active ingredient loss.
2Quantity of substance
If active ingredients are used in large quantities for everyday applications, then therapeutic potential is maximized, but cost increases due to scarcity and high price of these ingredients
Solution Approach 1:
The patent changes the absorption parameter from gastrointestinal (with liver metabolism) to oral mucosal absorption. This parameter change enables much higher quantities of active ingredient to be effectively utilized because direct mucosal absorption bypasses metabolic degradation, thereby maximizing therapeutic potential without wasting scarce ingredients.
3Reliability
If mucoadhesive tablet formulation is used, then direct absorption through oral mucosa is enabled, but manufacturing complexity increases
Solution Approach 1:
The patent employs a composite tablet formulation combining mucoadhesive polymers with phospholipids and active ingredients. This composite material approach enables direct oral mucosal absorption while maintaining a relatively simple manufacturing process, as the components are mixed and compressed into a single tablet without requiring complex multi-step fabrication.
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 formulation ensures efficient delivery and absorption of active ingredients, maximizing their therapeutic effects while minimizing metabolic loss.
Implementation Method 1
allows direct absorption through the oral mucosa, bypassing liver metabolism
Data Source
AI summary
The invention relates to a meltable tablet, in particular for use as a food supplement, comprising as main ingredients: - an active ingredient comprising one or more of berberine, spermidine, dehydroepiandrosterone, 5-hydroxytryptophan, royal jelly, propolis, polyene phosphatidylcholine, quercetin, dihydroquercetin, epigallocatechin gallate, α-lipoic acid and/or myrrh, - a disaccharide - a phosphatidylcholine