Urolithin A Medium-Chain Triglyceride Emulsion

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Solution Overview

Problem

Urolithins exhibit an unfavorable pharmacokinetic profile with multiple peaking in blood concentration and limited bioavailability when administered in simple saline suspension, making it difficult to optimize dosing and frequency of administration for effective health benefits, particularly in conditions related to mitochondrial activity and muscle function.

Innovation Solution

A composition comprising medium-chain triglycerides and a urolithin compound, such as Urolithin A, with specific particle size distribution, which improves bioavailability and pharmacokinetic profile by achieving a single peak in blood concentration, enhancing muscle function and treating various health conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If urolithins are administered in simple saline suspension, then the formulation is simple and easy to prepare, but the pharmacokinetic profile is unfavorable with multiple peaking in blood concentration and limited bioavailability

Engineering Contradiction:
Improveformulation simplicityVSAvoidpharmacokinetic profile
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent uses medium-chain triglycerides as an intermediary carrier substance to formulate urolithins. This mediator improves the pharmacokinetic profile by enabling single peak blood concentration and enhanced bioavailability, while maintaining formulation simplicity through a straightforward emulsion-based preparation method.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If urolithins are administered in simple saline suspension, then the formulation is easy to administer, but the bioavailability is limited and dosing optimization is difficult

Engineering Contradiction:
Improveadministration easeVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent changes the physical-chemical parameters of the formulation by using medium-chain triglycerides as the carrier instead of saline. This parameter change transforms the formulation into an emulsion system that improves bioavailability and enables single peak blood concentration, while maintaining ease of oral administration.

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If multiple peaking occurs in blood concentration, then the compound is absorbed in multiple gastrointestinal regions, but the dosing frequency and optimization become complex

Engineering Contradiction:
Improveabsorption distributionVSAvoiddosing regimen complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by pre-formulating urolithins with medium-chain triglycerides in a specific emulsion structure before administration. This pre-prepared formulation controls the release and absorption pattern to produce single peak blood concentration, thereby simplifying the dosing regimen to once or twice daily administration.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS11925616B2Compositions comprising urolithin compounds
Publication Date: 2024.03.12 AMAZENTIS SA
  • US11925616B2 patent drawing
  • US11925616B2 patent drawing
  • US11925616B2 patent drawing

AI summary

The invention provides compositions comprising a medium chain triglyceride and a urolithin. The invention also provides uses and methods associated with, or making use of the compositions, such as a medicament, dietary supplement, functional food or medical food and in the treatment and/or prophylaxis of a muscle-related pathological condition.