Iron-Carbohydrate Complex for Anemia Treatment

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Solution Overview

Problem

Current treatments for iron deficiency anemia, particularly oral iron(II) preparations, suffer from high toxicity and increased side effects, limiting their absorption and tolerance compared to iron(III) compounds, which are better absorbed but not suitable for parenteral administration.

Innovation Solution

Development of iron-carbohydrate complex compounds with a high proportion of iron(II) and low toxicity, where iron(II) is stabilized in a mixed valence state with iron(III), allowing for improved absorption and tolerance, especially when administered orally.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If iron(II) compounds are administered orally, then absorption is faster, but toxicity and side effects increase

Engineering Contradiction:
Improveabsorption speedVSAvoidtoxicity and side effects
Core Design Contradiction:
SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent uses carbohydrate molecules as intermediaries to form complexes with iron(II), which stabilize the iron in a mixed valence state with iron(III). This intermediary complex reduces the toxicity and side effects of pure iron(II) compounds while maintaining rapid absorption characteristics, effectively mediating between the beneficial absorption speed and harmful toxicity effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the oxidation state parameter of iron from pure divalent iron(II) to a mixed valence state containing both iron(II) and iron(III). This parameter change allows the iron compound to exhibit both rapid absorption (from iron(II)) and reduced toxicity (from iron(III) stabilization), resolving the contradiction between absorption speed and harmful effects

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If iron(III) compounds are administered, then toxicity is reduced, but absorption speed decreases

Engineering Contradiction:
ImprovetoxicityVSAvoidabsorption speed
Core Design Contradiction:
Object-affected harmful factorsVSSpeed

Solution Approach 1:

The patent changes the oxidation state parameter from pure trivalent iron(III) to a mixed valence state containing both iron(II) and iron(III). This parameter change enables the compound to maintain reduced toxicity (through iron(III) stabilization) while achieving rapid absorption (through iron(II) presence), thus resolving the contradiction between low toxicity and fast absorption

Inventive Principle:
Principle #35Parameter changes

3Speed

If pure iron(II) preparations are used, then absorption is rapid, but tolerability decreases due to high toxicity

Engineering Contradiction:
Improveabsorption speedVSAvoidtolerability
Core Design Contradiction:
SpeedVSEase of operation

Solution Approach 1:

The patent introduces carbohydrate molecules as intermediaries that form stable complexes with iron(II), stabilizing it in a mixed valence state. This intermediary complex maintains the rapid absorption characteristic of iron(II) while significantly improving tolerability by reducing the high toxicity associated with pure iron(II) preparations

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite iron-carbohydrate complex compound combining iron(II) with carbohydrate molecules. This composite material exhibits both rapid absorption (from the iron(II) component) and improved tolerability (from the stabilizing effect of carbohydrates and mixed valence state), resolving the contradiction between absorption speed and tolerability

Inventive Principle:
Principle #40Composite materials

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-carbohydrate complex compounds achieve rapid and well-tolerated iron absorption, reducing toxicity and side effects, making them suitable for both oral and parenteral administration, with enhanced therapeutic efficacy for iron deficiency anemia treatment.

Implementation Method 1

The invention relates to iron-carbohydrate complex compounds containing iron(III) and iron(II)... These are therefore so-called 'mixed valence' compounds, in which the metal is present in several oxidation states simultaneously

Methodology Applied
Scientific EffectRedox reaction: Redox Reactions

Implementation Method 2

in which the carbohydrates are partially complexed and/or bound via hydrogen bonds

Methodology Applied
Scientific EffectHydrogen bonding:

Implementation Method 3

The invention was thus based on the objective of providing an improved drug formulation that allows for particularly good absorption of iron by the body, especially when administered orally

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentEP2111416B2Iron-hydrocarbon complex compounds
Publication Date: 2022.03.30 VIFOR (INT) AG

AI summary

The invention relates to an iron-hydrocarbon complex compound which is characterized by an iron (II) content. The invention also relates to methods for producing said iron-hydrocarbon complex compound as well as the use thereof for the treatment of iron deficiency anemia.