Thermoformed Triterpene Extrudates for Solubility and Bioavailability

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Solution Overview

Problem

Current formulations of triterpenes and triterpenoids suffer from low solubility, dispersion, and bioavailability due to their poor solubility and dispersibility in aqueous solutions, leading to low bioaccessibility and cumbersome manufacturing processes.

Innovation Solution

A composition comprising triterpenes/triterpenoids in the form of a thermoformed extrudate with a first amorphous phase and optionally a second crystalline phase, dispersed in natural or synthetic proteins, oligosaccharides, or polysaccharides, produced through hot extrusion, enhancing solubility and dispersion in aqueous media.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cosmetics containing hydroquinone, mercury, or high concentrations of vitamin C are used to treat melasma, then skin lightening effect is achieved, but skin irritation and safety issues occur

Engineering Contradiction:
ImprovesafetyVSAvoidskin irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and eliminates harmful substances (hydroquinone, mercury, high concentration vitamin C) from conventional melasma treatments, replacing them with safe triterpene derivatives that provide effective skin lightening without causing irritation or safety concerns

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the chemical parameters by using specific concentrations of triterpene derivatives (0.01-10% w/w) and their combinations, achieving both safety and efficacy by optimizing the concentration parameters away from harmful thresholds while maintaining therapeutic effect

Inventive Principle:
Principle #35Parameter changes

2Reliability

If natural plant extracts are used to treat melasma, then safety is improved, but treatment efficacy is insufficient

Engineering Contradiction:
ImprovesafetyVSAvoidtreatment efficacy
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent creates composite formulations combining multiple triterpene derivatives from different natural sources (oleanolic acid, ursolic acid, betulinic acid, maslinic acid) with synergistic effects, achieving enhanced treatment efficacy while maintaining the safety profile of natural extracts

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent merges multiple triterpene compounds with different mechanisms of action into a single formulation, combining their individual benefits to achieve superior overall efficacy in treating melasma while preserving safety

Inventive Principle:
Principle #5Merging (Combining)

3Productivity

If topical treatments are applied frequently to achieve better melasma results, then treatment efficacy improves, but skin barrier function deteriorates

Engineering Contradiction:
Improvetreatment efficacyVSAvoidskin barrier function
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent uses triterpene derivatives that act rapidly and effectively at lower concentrations, allowing for less frequent application compared to conventional treatments, thereby reducing cumulative irritation while maintaining treatment efficacy through optimized formulation

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Data Source

PatentEP3989943B1Composition comprising at least one triterpene and/or at least one triterpenoid and/or at least one of the glycosylated forms thereof
Publication Date: 2026.05.20 TILMAN GMBH
  • EP3989943B1 patent drawingFigure 1~2
  • EP3989943B1 patent drawingFigure 3~4
  • EP3989943B1 patent drawingFigure 5~6

AI summary

The present invention relates to a composition in the form of a thermoformed extrudate comprising at least one triterpene and/or at least one triterpenoid and/or at least one of the glycosylated forms thereof and at least one polymer chosen from the group consisting of natural or synthetic proteins, natural or synthetic oligosaccharides, natural or synthetic polysaccharides, derivatives thereof and mixtures thereof, said at least one triterpene and/or said at least one triterpenoid and/or said at least one of the glycosylated forms thereof comprising at least one amorphous first phase and optionally one crystalline second phase. The present invention also relates to the process for manufacturing such a composition by thermoforming and to the use of such a composition.