Transdermal Fentanyl Solution for Equine Pain Control

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Solution Overview

Problem

The use of opioids, particularly fentanyl, in veterinary medicine is limited by poor oral bioavailability and rapid clearance, leading to short duration of action and undesirable side effects in equines, and existing transdermal patch formulations face regulatory and pharmacokinetic challenges.

Innovation Solution

A transdermal pharmaceutical solution formulation of fentanyl combined with a penetration enhancer and a volatile liquid is used, allowing for deposition in the stratum corneum for prolonged systemic absorption, overcoming bioavailability and duration limitations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If transdermal patch formulation is used to deliver fentanyl to equines, then non-invasive dosing and continuous drug delivery are achieved, but slow delivery rate and low extent of fentanyl delivery occur

Engineering Contradiction:
Improvenon-invasive dosingVSAvoiddelivery rate
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The patent changes the physical and chemical parameters of the transdermal formulation by incorporating specific penetration enhancers (such as fatty acids, fatty acid esters, or glycolic acid) and adjusting the vehicle composition to optimize fentanyl permeation through the equine skin barrier, thereby increasing delivery rate while maintaining non-invasive administration

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces penetration enhancers as intermediary substances that facilitate fentanyl transport across the skin barrier. These enhancers act as mediators between the fentanyl and the skin permeation pathway, increasing the extent and rate of drug delivery without requiring invasive administration

Inventive Principle:
Principle #24Intermediary (Mediator)

2Duration of action of stationary object

If traditional transdermal patch formulation is used, then continuous drug delivery is achieved, but regulatory approval and pharmacovigilance are insufficient

Engineering Contradiction:
Improveduration of actionVSAvoidregulatory approval
Core Design Contradiction:
Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent modifies the formulation parameters by specifying precise concentration ranges (fentanyl 0.01-10%, penetration enhancer 1-20%, vehicle 70-70%) and physical properties to create a standardized, regulatory-compliant product that maintains prolonged duration of action while meeting veterinary medical standards for safety and monitoring

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If fentanyl is administered to equines, then pain management is achieved, but dose dependent CNS excitation and gastrointestinal stasis occur

Engineering Contradiction:
Improvepain controlVSAvoidCNS excitation
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent achieves continuous, steady-state fentanyl delivery through the transdermal formulation, eliminating peak plasma concentrations that cause CNS excitation. The penetration enhancers ensure consistent permeation rates, maintaining therapeutic pain management without the harmful peak-trough fluctuations associated with intermittent administration

Inventive Principle:
Principle #20Continuity of useful action

4Productivity

If transdermal patch is applied to equine skin, then fentanyl delivery is achieved, but patch damage and consumption leading to toxicity are possible

Engineering Contradiction:
Improvefentanyl deliveryVSAvoidtoxicity from consumption
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent formulates the transdermal system as a disposable application that is not intended for prolonged wear or repeated use. The formulation is designed to be applied and then discarded, eliminating the risk of patch consumption and subsequent toxicity that would occur with reusable or long-lasting patches

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

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

This approach results in faster, more extensive, and higher absorption rates of fentanyl in equines, reducing the required therapeutic dose, minimizing side effects, and improving safety and regulatory compliance compared to traditional patch formulations.

Implementation Method 1

the dermal barrier to drug permeation can be overcome in equines by using a transdermal pharmaceutical formulation... deposition of fentanyl in the stratum corneum of an equine followed by prolonged systemic absorption

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentEP2675454B1Methods for controlling pain in equines using a transdermal solution of fentanyl
Publication Date: 2020.01.22 AUDEVARD
  • EP2675454B1 patent drawingFigure 1
  • EP2675454B1 patent drawingFigure 2~2A
  • EP2675454B1 patent drawingFigure 3

AI summary

This invention provides methods of controlling pain in an equine for an effective period of time comprising transdermally administering a composition comprising fentanyl, a penetration enhancer, and a volatile liquid, wherein the composition is a solution. The invention also provides a single unit dose of the composition.