Inorganic Nitrite Formulation for Neuropathic Pain Relief

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for neuropathic pain, particularly in conditions like diabetic peripheral neuropathy, are inadequate in providing sustained relief without associated chronic ischemia, and there is a need for therapeutic strategies that modulate nitric oxide levels for pain management.

Innovation Solution

A tablet or capsule formulation of 40 mg inorganic nitrite (NaNO2 or KNO2) with pharmaceutically acceptable excipients for sustained release, administered orally twice a day to reduce neuropathic pain, potentially combined with other agents like NSAIDs or antidepressants, to modulate brain function and alleviate pain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If inorganic nitrite is administered to treat neuropathic pain, then pain intensity and frequency are reduced, but the risk of inducing chronic ischemia increases

Engineering Contradiction:
Improveneuropathic painVSAvoidchronic ischemia
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent changes the dosage parameter to 40 mg of inorganic nitrite, which is specifically optimized to provide analgesic effects while remaining below the threshold that would induce chronic ischemia. This parameter adjustment resolves the contradiction by finding the optimal dose level that maximizes pain relief while minimizing adverse effects.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If nitric oxide levels are increased to modulate pain pathways, then neuropathic pain is alleviated, but the complexity of dosing and administration increases

Engineering Contradiction:
Improveneuropathic painVSAvoiddosing regimen
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent establishes a simple twice-daily dosing regimen with a fixed 40 mg dose, which simplifies administration while maintaining effective nitric oxide modulation for pain relief. This standardized parameter approach reduces dosing complexity compared to more frequent or variable dosing schedules.

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 formulation provides effective reduction in pain intensity, frequency, and duration, improving quality of life for subjects with neuropathic pain, including diabetic peripheral neuropathy, by maintaining nitric oxide levels and addressing underlying pain mechanisms.

Implementation Method 1

Nitric oxide (NO) serves as a neurotransmitter between nerve cells... The NO-cGMP cascade is involved in learning and memory through the maintenance of long-term potentiation (LTP)

Methodology Applied
Scientific EffectNitrite to nitric oxide conversion: Redox Reactions

Data Source

PatentEP2958573B1Pharmaceutical formulations of nitrite and uses thereof
Publication Date: 2019.05.08 THE BOARD OF SUPERVISORS OF THE LOUISIANA STATE UN
  • EP2958573B1 patent drawingFigure 1A~1B
  • EP2958573B1 patent drawingFigure 2A~2B
  • EP2958573B1 patent drawing

AI summary

The present invention relates to pharmaceutical compositions of nitrites such as inorganic nitrites, or any pharmaceutically acceptable salts, solvates, or prodrugs thereof, and the medical use of these compositions. The pharmaceutical compositions, which can be formulated for oral administration, can provide immediate release or extended release of the nitrite ion (NO2 -)The pharmaceutical compositions of the invention are useful, for example, for modulating brain function, in particular improving mood and/or psychological state, in the treatment of disorders of brain development, and in the treatment and/or reduction of pain.