Neuropathy Composition Synergy CB2 Receptor Pain Relief

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for peripheral neuropathy and associated pain, particularly neuropathic and mixed pain, are inadequate due to limited clinical benefits and undesirable side effects from traditional analgesics, necessitating the development of a more effective therapy.

Innovation Solution

A composition comprising palmitoylethanolamide as an endocannabinoid, β-caryophyllene as a phytoterpene, and a mixture of alpha-lipoic acid and vitamin D, which synergistically acts on CB2 receptors to enhance analgesic and anti-inflammatory effects, improving pain management for neuropathic and mixed pain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional analgesics are used for neuropathic pain, then pain relief is provided, but clinical benefits are limited and undesired side effects occur

Engineering Contradiction:
Improveclinical benefitVSAvoidundesired side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies the composite materials principle by formulating a multi-component nutraceutical composition containing palmitoylethanolamide, α-lipoic acid, vitamin D3, and β-caryophyllene. This composite approach combines substances with complementary mechanisms of action: palmitoylethanolamide modulates the endocannabinoid system and PPAR-α receptors, α-lipoic acid provides antioxidant support and nerve regeneration, vitamin D3 addresses neurotrophic factors, and β-caryophyllene acts on CB2 receptors. The synergistic interaction of these components achieves superior analgesic efficacy for neuropathic pain while maintaining a favorable safety profile without the harmful side effects associated with traditional analgesics.

Inventive Principle:
Principle #40Composite materials

2Reliability

If multiple drugs are administered for neuropathic pain, then pain control is attempted, but treatment complexity increases and side effects accumulate

Engineering Contradiction:
Improvepain controlVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies the merging principle by consolidating multiple therapeutic agents into a single integrated nutraceutical formulation. Instead of requiring separate administration of antidepressants, antiepileptics, or opioids, the composition combines palmitoylethanolamide, α-lipoic acid, vitamin D3, and β-caryophyllene in one product. This unified approach simplifies the treatment regimen, improves patient compliance, and enables synergistic interactions between components while avoiding the cumulative side effects of polypharmacy.

Inventive Principle:
Principle #5Merging (Combining)

3Ease of manufacture

If conventional therapies are used, then standard treatment is provided, but effectiveness for neuropathic pain is insufficient

Engineering Contradiction:
Improvetreatment availabilityVSAvoidanalgesic effectiveness
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent applies the parameter changes principle by shifting from conventional pharmacological parameters (opioid receptors, monoamine reuptake inhibition) to alternative biological parameters involving the endocannabinoid system, PPAR-α receptors, and antioxidant pathways. By utilizing naturally occurring substances like palmitoylethanolamide and α-lipoic acid that act through these different mechanisms, the composition achieves effective neuropathic pain control through novel pathways not engaged by traditional analgesics, thereby improving effectiveness while maintaining ease of manufacture as a nutraceutical product.

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 composition significantly boosts anti-inflammatory action and improves analgesic effects on neuropathic and mixed pain, offering a more effective treatment option with reduced side effects compared to traditional therapies.

Implementation Method 1

A composition comprising at least one endocannabinoid being palmitoylethanolamide, at least one phytoterpene being β-caryophyllene, and at least one component selected from mixtures of alpha-lipoic acid and vitamin D

Methodology Applied
Scientific EffectEndocannabinoid receptor binding:

Implementation Method 2

at least one phytoterpene being β-caryophyllene, and at least one component selected from mixtures of alpha-lipoic acid and vitamin D, which synergistically acts on CB2 receptors to enhance analgesic and anti-inflammatory effects

Methodology Applied
Scientific EffectPhytoterpene receptor binding:

Implementation Method 3

at least one component selected from mixtures of alpha-lipoic acid and vitamin D

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Data Source

PatentEP3773526B1Composition for the treatment of peripheral neuropathies
Publication Date: 2024.07.17 SOCHIM INT SPA

AI summary

A composition is disclosed for the treatment of peripheral neuropathy, in particular the pain associated therewith and mixed pain. In particular, the composition according to the invention comprises at least one endocannabinoid, at least one phytoterpene, and at least one component selected from alpha-lipoic acid, vitamin D and mixtures thereof, which have been shown to be significantly effective as adjuvants in the treatment of the inflammation underlying neuropathic and mixed pain.