Iron(III)-3-hydroxy-isonicotinamide Complexes for Iron Deficiency

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Solution Overview

Problem

Current iron complexes for treating iron deficiency symptoms and anemias often suffer from low stability, solubility issues, and high toxicity, particularly with iron(II) salts causing oxidative stress, and polymeric complexes have limited oral application efficacy.

Innovation Solution

Development of iron(III)-3-hydroxy-isonicotinamide complex compounds with high water solubility and stability at neutral pH, allowing direct uptake into intestinal cells and release of iron without forming free iron ions, reducing oxidative stress and side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If iron(II) salts are used for treating iron deficiency, then iron supplementation is achieved, but oxidative stress and high toxicity occur

Engineering Contradiction:
Improveiron supplementationVSAvoidoxidative stress and toxicity
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses iron(III) complex compounds with 3-hydroxy-isonicotinamide ligands as intermediary compounds that deliver iron to the body without causing oxidative stress. These complexes act as mediators between the iron source and the body's iron metabolism, releasing iron in a controlled manner that avoids the harmful effects of direct iron(II) salt administration while maintaining therapeutic efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the oxidation state parameter from iron(II) to iron(III) and modifies the chemical environment through specific ligand coordination. This parameter change transforms the properties of iron compounds, eliminating oxidative stress while preserving iron supplementation benefits. The complexes exhibit enhanced stability and reduced toxicity compared to traditional iron(II) salts.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If polymeric iron complexes are used, then iron delivery is improved, but oral application efficacy is limited

Engineering Contradiction:
Improveiron deliveryVSAvoidoral application efficacy
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent employs low-molecular-weight iron(III) complex compounds with specific local chemical properties that facilitate oral absorption. These compounds have optimized molecular characteristics including appropriate size, charge distribution, and ligand structure that enable them to interact effectively with intestinal transport mechanisms, overcoming the absorption limitations of polymeric complexes while maintaining stable iron delivery.

Inventive Principle:
Principle #3Local quality

3Stability of the object's composition

If iron complexes are designed for high stability, then iron retention is improved, but solubility issues occur

Engineering Contradiction:
Improveiron complex stabilityVSAvoidwater solubility
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The invention optimizes multiple parameters simultaneously: the oxidation state (iron(III)), the ligand structure (3-hydroxy-isonicotinamide with specific substituents), and the molecular weight. These parameter changes create a balance where the complexes maintain high stability through strong iron-ligand bonding while the specific ligand properties and molecular characteristics ensure adequate water solubility for oral administration.

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 iron(III)-3-hydroxy-isonicotinamide complexes demonstrate enhanced iron utilization, faster therapeutic effects, reduced side effects, and improved stability, making them suitable for effective oral treatment of iron deficiency symptoms and anemias without the drawbacks of traditional iron salts.

Implementation Method 1

Development of iron(III)-3-hydroxy-isonicotinamide complex compounds with high water solubility and stability at neutral pH, allowing direct uptake into intestinal cells and release of iron without forming free iron ions

Methodology Applied
Scientific EffectComplex formation: Chemical Bonding

Data Source

PatentUS9248134B1Fe(III) complex compounds for the treatment and prophylaxis of iron deficiency symptoms and iron deficiency anemias
Publication Date: 2016.02.02 VIFOR (INT) AG

AI summary

The invention relates to iron(III) complex compounds and pharmaceutical compositions comprising them for the use as medicaments, in particular for the treatment and/or prophylaxis of iron deficiency symptoms and iron deficiency anemias.