Beta-Alanine Formulations with NMDA Modulators for Paraesthesia Control

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Solution Overview

Problem

The administration of β-alanine for improving exercise performance is limited by the occurrence of sensory paraesthesia at doses above 10 mg/kg, which becomes severe at 40 mg/kg, making it difficult to achieve peak physical performance effects within a reasonable timeframe due to dosage restrictions.

Innovation Solution

Compositions and formulations that combine β-alanine with agents that modulate the N-methyl D-aspartate (NMDA) pathway, such as L-theanine, GABA, or NMDA receptor antagonists, to enhance tolerance and reduce paraesthesia, allowing for higher doses to be administered over a shorter period.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If higher doses of β-alanine are administered to achieve peak physical performance effects faster, then productivity is improved, but sensory paraesthesia becomes severe making the treatment intolerable

Engineering Contradiction:
Improvetime to achieve peak physical performanceVSAvoidsensory paraesthesia
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces NMDA pathway modulators as intermediary substances that mediate between β-alanine and the sensory nervous system. These modulators block or attenuate the transmission of paraesthetic signals while allowing β-alanine to exert its performance-enhancing effects, thus resolving the contradiction between dosage effectiveness and tolerability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the harmful paraesthetic sensation into a beneficial outcome by using NMDA modulators to block the harmful sensory pathway while preserving or enhancing the performance benefits of β-alanine. The harmful high-dose paraesthesia is transformed into a tolerable or even beneficial supplementation approach

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

2Duration of action of moving object

If higher doses of β-alanine are administered to reduce supplementation time, then duration of action is improved, but the harmful effect of paraesthesia increases

Engineering Contradiction:
Improvesupplementation time periodVSAvoidparaesthesia
Core Design Contradiction:
Duration of action of moving objectVSObject-generated harmful factors

Solution Approach 1:

NMDA pathway modulators serve as intermediary agents that selectively block the harmful sensory transmission pathway while allowing the beneficial metabolic effects of β-alanine to proceed. This enables shorter supplementation periods with higher doses without experiencing severe paraesthesia

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physiological parameters of sensory perception by modulating NMDA receptor activity. This parameter change in the sensory pathway allows for altered tolerance thresholds, enabling higher doses to be administered for shorter periods without crossing the paraesthesia threshold

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2948139B1Methods of improving tolerability, pharmacodynamics, and efficacy of b-alanine and use therefor
Publication Date: 2019.06.12 LOPEZ HECTOR L
  • EP2948139B1 patent drawingFigure 1
  • EP2948139B1 patent drawingFigure 2
  • EP2948139B1 patent drawingFigure 3

AI summary

The present invention relates in some aspects to compositions (e.g., pharmaceutical, nutritional compositions, etc.), formulations, and food or beverage products comprising, consisting essentially of, or consisting of (a) β-alanine or a derivative of β-alanine, and (b) at least one agent that inhibits the N-methyl D- aspartate (NMDA) pathway or a pathway which converges downstream with the NMDA pathway. The compositions, formulations, and food or beverage products are useful for enhancing physical performance, reducing β-alanine- induced paraesthesia, and improving tolerance and compliance to higher doses of β-alanine, thereby reducing the length of time it takes to achieve peak effect of β- alanine, and increasing the magnitude of peak effect on physical performance in a human or animal.