Repeated High-Concentration Capsaicin Patch Application for Neuropathic Pain Non-Responders

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Solution Overview

Problem

A significant number of patients do not respond to topical treatment with high-concentration capsaicin patches or creams for neuropathic pain, and there is a need for medicaments that can provide pain relief to these non-responders.

Innovation Solution

High-concentration capsaicin and/or capsaicinoid topical dose units or patches with concentrations of at least 2.5 wt.-%, preferably 5 wt.-%, are repeatedly applied to patients who did not initially respond to capsaicin treatment, converting them into responders and achieving pain relief exceeding 30% versus baseline.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high-concentration capsaicin patches are applied to patients with neuropathic pain, then pain relief is achieved in responders, but a significant number of patients do not respond to the treatment

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidapplicability to non-responder population
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies periodic re-treatment with high-concentration capsaicin patches to patients who initially did not respond. The treatment is administered in cycles, allowing the nervous system to reset and become responsive again. This periodic application converts non-responders into responders over time, addressing the limitation of initial treatment failure while maintaining the effectiveness of the high-concentration formulation.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The patent employs a preliminary low-concentration capsaicin treatment phase before administering the high-concentration patch. This preliminary action sensitizes the TRPV1 receptors and prepares the nervous system for subsequent high-concentration treatment, thereby increasing the likelihood of response in patients who would otherwise be non-responders.

Inventive Principle:
Principle #10Preliminary action

2Adaptability or versatility

If repeated applications of high-concentration capsaicin patches are administered to convert non-responders into responders, then responder rates increase, but treatment time and number of applications increase

Engineering Contradiction:
Improveresponder rateVSAvoidtreatment duration
Core Design Contradiction:
Adaptability or versatilityVSLoss of time

Solution Approach 1:

The preliminary low-concentration treatment phase prepares patients for faster response to subsequent high-concentration treatments. By pre-sensitizing the TRPV1 receptors, this preliminary action reduces the number of high-concentration patch applications needed, thereby缩短ing the overall treatment duration while maintaining high responder rates.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The structured periodic treatment protocol with defined intervals between applications optimizes the conversion of non-responders to responders. The timing is calibrated to allow sufficient recovery and receptor reset while maintaining treatment momentum, balancing the need for multiple applications with the goal of minimizing total treatment time.

Inventive Principle:
Principle #19Periodic action

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

Repeated topical administration of high-concentration capsaicin increases responder rates among initial non-responders, with over a third converting into responders, and provides sustained pain relief for up to 90 days or longer, with improved response rates when subsequent applications are made within 84 days.

Implementation Method 1

Capsaicin is a highly selective agonist for the transient receptor potential vanilloid 1 receptor (TRPV1). The initial effect of capsaicin is the activation of TRPV1-expressing cutaneous nociceptors

Methodology Applied
Scientific EffectTRPV1 receptor activation:

Implementation Method 2

Following capsaicin exposure, cutaneous nociceptors become less sensitive to a variety of stimuli. These later-stage effects of capsaicin are frequently referred to as 'desensitization' and are thought to underlie the pain relief.

Methodology Applied
Scientific EffectDesensitization:

Implementation Method 3

Further preferred aspects of treating neuropathic conditions according to the invention involve regenerating and/or restoring sensory nerve fibers

Methodology Applied
Scientific EffectNerve fiber regeneration:

Data Source

PatentUS20230157977A1Repeated topical application of capsaicin patch for treating initial non-responders
Publication Date: 2023.05.25 AVERITAS PHARMA INC
  • US20230157977A1 patent drawing

AI summary

The invention relates to repeated treatment of a neuropathic condition, preferably peripheral neuropathic pain, by application of one or more high-concentration capsaicin and/or capsaicinoid topical dose units, preferably high-concentration capsaicin and/or capsaicinoid patches, to patients who previously did not respond or insufficiently responded to a previous application of one or more high-concentration capsaicin and/or capsaicinoid topical dose units, preferably high-concentration capsaicin and/or capsaicinoid patches or any other high-concentration capsaicin and/or capsaicinoid formulation previously topically administered.