Oxycodone and Palmitoylethanolamine Combination for Opioid Side Effects

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Solution Overview

Problem

Current opioid therapies face challenges in minimizing side effects such as irritation, confusion, and uncontrolled movement associated with oxycodone use, while also dealing with opioid dependence and addiction, and there is a need for compositions that enhance opioid potency and safety.

Innovation Solution

Pharmaceutical compositions combining oxycodone with N-acylethanolamines, specifically palmitoylethanolamine (PEA), in specific molar ratios for systemic administration, which potentiates the therapeutic effect of opioids and reduces side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If oxycodone is administered to achieve analgesic effect, then pain relief is improved, but side effects such as irritation, confusion, and uncontrolled movement increase

Engineering Contradiction:
Improveanalgesic effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces N-acylethanolamines as intermediary substances that mediate between oxycodone and the body's neural system. These intermediaries modulate opioid receptor activation, providing analgesic effects while reducing harmful side effects through balanced receptor interaction.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite pharmaceutical formulation combining oxycodone with N-acylethanolamines in specific ratios. This composite approach leverages the synergistic effects of both substances, where N-acylethanolamines enhance opioid potency while simultaneously reducing side effects through their own pharmacological properties.

Inventive Principle:
Principle #40Composite materials

2Reliability

If oxycodone dosage is increased to enhance therapeutic potency, then pain relief is improved, but risk of addiction and dependence increases

Engineering Contradiction:
Improvetherapeutic potencyVSAvoidaddiction risk
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the compositional parameters of the pharmaceutical formulation by incorporating N-acylethanolamines alongside oxycodone. This parameter modification allows for reduced oxycodone dosage while maintaining therapeutic potency, thereby lowering addiction risk through decreased exposure to the addictive substance.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

N-acylethanolamines serve as intermediary agents that enhance the therapeutic effects of lower oxycodone doses. By mediating the pharmacological response, they allow effective pain management at reduced opioid levels, minimizing the development of dependence and addiction.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If oxycodone is used to treat pain, then analgesic effect is achieved, but required dosage is high leading to increased side effects

Engineering Contradiction:
Improveanalgesic effectVSAvoidrequired dosage
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent merges oxycodone with N-acylethanolamines in a combined pharmaceutical formulation. This merging creates a synergistic effect where the total analgesic potency is enhanced, allowing for reduced oxycodone dosage while maintaining or improving pain relief effectiveness.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The composite formulation of oxycodone and N-acylethanolamines creates a more potent therapeutic agent per unit dose. This composite material approach increases the effective concentration of analgesic activity, reducing the quantity of oxycodone needed to achieve the desired therapeutic effect.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3297622B1Combinations of oxycodone and n-acylethanolamine palmitoylethanolamine for reducing opioid-associated side effects
Publication Date: 2023.11.01 SCISPARC LTD
  • EP3297622B1 patent drawingFigure 1
  • EP3297622B1 patent drawingFigure 2
  • EP3297622B1 patent drawingFigure 3A

AI summary

The present invention provides pharmaceutical compositions comprising opioids and N-acylethanolamines, and methods for their use in preventing and treating a variety of opioid- responsive conditions and opioid-related side-effects.