Orodispersible Tablet Composition for Bypassing First-Pass Metabolism

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Solution Overview

Problem

There is a need for active ingredients like cordycepin, curcumin, omega-3, melatonin, vitamin C, ubiquinone-10, resveratrol, and other nutrients to be made more readily available and easier to use in large quantities due to their scarcity and high price, with existing formulations not effectively bypassing the liver's first-pass effect.

Innovation Solution

An orodispersible tablet formulation comprising an active ingredient, disaccharide trehalose, and phosphatidylcholine (lecithin) that dissolves in the oral cavity, allowing direct absorption through the mucosa and bypassing the liver's first-pass effect.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional oral formulations are used, then the active ingredients can be administered, but they undergo first-pass metabolism in the liver which reduces their bioavailability and therapeutic effectiveness

Engineering Contradiction:

ImprovebioavailabilityVSAvoidfirst-pass metabolism loss

Core Design Contradiction:

ReliabilityVSLoss of energy

Solution Approach 1:

The patent uses disaccharide trehalose as an intermediary carrier that facilitates direct absorption of active ingredients through the oral mucosa, bypassing the liver's first-pass metabolism. Trehalose forms a complex with the active ingredient that can be directly absorbed by mucosal cells, acting as a mediator to deliver the active ingredient to the bloodstream without hepatic degradation.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the conventional gastrointestinal absorption mechanism (which passes through the liver) with a direct mucosal absorption mechanism. By using trehalose-based orodispersible tablets that dissolve in the oral cavity, the active ingredient is absorbed directly through the mucosa into the bloodstream, substituting the traditional hepatic first-pass metabolism pathway.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Quantity of substance

If large quantities of active ingredients are provided to maximize therapeutic effect, then the therapeutic potential is increased, but the scarcity and high price of these products makes this difficult

Engineering Contradiction:

Improveamount of active ingredientVSAvoidavailability and cost

Core Design Contradiction:

Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent changes the administration parameter from conventional oral ingestion to direct mucosal absorption via orodispersible tablet. This parameter change in the delivery mechanism allows for more efficient utilization of the active ingredient, reducing waste and maximizing therapeutic effect from smaller quantities, thereby addressing the scarcity issue.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a model system using disaccharide trehalose as a carrier that can be easily synthesized and used to formulate orodispersible tablets. This copying approach allows for cost-effective production of the delivery system, making it economically viable to provide large quantities of expensive active ingredients while maintaining affordability.

Inventive Principle:

Principle #26Copying

3Speed

If the tablet formulation is designed to dissolve quickly in the oral cavity for direct absorption, then the therapeutic effectiveness is improved, but the stability and shelf life may be compromised

Engineering Contradiction:

Improvedissolution speedVSAvoidshelf life

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent employs a composite material system consisting of disaccharide trehalose, phosphatidylcholine, and the active ingredient. This composite formulation provides both rapid dissolution properties for direct absorption and enhanced stability through the protective effect of the phosphatidylcholine and trehalose matrix, allowing the tablet to maintain its structural integrity during storage while dissolving quickly in the oral cavity during use.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent utilizes the phase transition properties of phosphatidylcholine, which changes from a solid crystalline structure during storage to a more fluid state in the oral cavity. This parameter change enables the tablet to maintain stability during shelf life while achieving rapid dissolution and absorption in the mouth, resolving the contradiction between stability and speed.

Inventive Principle:

Principle #35Parameter changes

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 directly into the bloodstream, maximizing therapeutic potential while avoiding liver metabolism and ensuring stability and shelf life.

Implementation Method 1

dissolves in the oral cavity, allowing direct absorption through the mucosa and bypassing the liver's first-pass effect

Methodology Applied

Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentUS20260034057A1Orodispersible tablet, in particular for use as a food supplement

Publication Date: 2026.02.05 GOETHE BIOTECHNOLOGY SWISS AG

AI summary

An orodispersible tablet, in particular for use as a dietary supplement, comprising as main ingredients: an active agent, a disaccharide, and a phosphatidylcholine.