Capsaicinoid Topical Composition with Extended Release Agent

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Solution Overview

Problem

Current capsaicin-based pain relief products often cause severe burning and stinging sensations, leading to poor patient compliance and inadequate pain relief due to low concentrations and delayed therapeutic effects.

Innovation Solution

A topical composition containing 0.075-20% capsaicinoid, an extended release agent like hyaluronic acid, and a surfactant to slow the release and reduce burning sensations, allowing for higher capsaicin concentrations without severe side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If higher concentrations of capsaicin are used to improve pain relief efficacy, then the therapeutic effect is enhanced, but the burning and stinging sensations become more severe

Engineering Contradiction:

Improvepain relief efficacyVSAvoidburning and stinging sensations

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The capsaicin delivery is segmented into controlled release phases through the use of hydrogel matrix and microneedle array, which divides the drug release into sustained portions rather than immediate delivery, thereby maintaining therapeutic efficacy while reducing peak concentration-related side effects

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The hydrogel serves as an intermediary carrier that mediates between the capsaicin drug and the skin tissue, controlling the release kinetics and reducing direct irritation. The microneedles act as intermediaries to deliver the hydrogel-capsaicin complex through the stratum corneum barrier in a controlled manner

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of moving object

If prolonged treatment is required to achieve therapeutic effect, then the pain relief duration is extended, but patient compliance deteriorates due to extended exposure to burning sensations

Engineering Contradiction:

Improvetherapeutic effect durationVSAvoidpatient compliance

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

The microneedles create preliminary microchannels in the stratum corneum before capsaicin delivery, enabling enhanced and sustained drug penetration. This preliminary physical modification allows for prolonged therapeutic action while controlling the release profile to minimize irritation during the treatment period

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The hydrogel matrix provides continuous capsaicin release over an extended period, maintaining therapeutic efficacy continuously. This sustained delivery ensures prolonged pain relief while the controlled release rate prevents acute irritation, improving patient compliance throughout the treatment duration

Inventive Principle:

Principle #20Continuity of useful action

3Object-affected harmful factors

If low concentrations of capsaicin are used to reduce burning sensations, then patient tolerability improves, but the therapeutic effect becomes inadequate

Engineering Contradiction:

Improveburning sensation intensityVSAvoidpain relief effectiveness

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The delivery system dynamically controls capsaicin release through the hydrogel-microneedle combination, adjusting the effective delivery rate and concentration profile over time. This dynamic release pattern maintains lower irritation levels while ensuring sufficient therapeutic exposure through sustained action

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The system changes the physical parameters of drug delivery by using microneedles to bypass the stratum corneum barrier and hydrogel to control release kinetics. This parameter change enables effective delivery of capsaicin at concentrations and rates that would otherwise be contradictory, achieving both tolerability and efficacy

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 provides long-term pain relief with reduced burning and stinging, making it more tolerable for extended use and achieving higher capsaicin concentrations without diminishing tactile sensation.

Implementation Method 1

an extended release agent to slow the release of said capsaicinoid from said composition upon administration of said composition to a mammal

Methodology Applied

Scientific EffectExtended release:

Implementation Method 2

a surfactant, wherein said composition reduces or eliminates the burning and stinging created by said capsaicinoid upon topical administration

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Data Source

PatentUS11737994B2Topical compositions for pain relief, manufacture and use

Publication Date: 2023.08.29 JIANGSU AOSAIKANG PHARMA CO LTD

AI summary

The present invention relates to TRPV1 selective agonist compositions including a capsaicinoid, a surfactant and an extended release agent, and to methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.