FeII-Ascorbate-Proteinate Complex Oral Iron Formulation

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Solution Overview

Problem

Current treatments for iron deficiency anemia are limited by side effects such as gastric damage and unpleasant taste, and existing formulations have challenges with bioavailability and absorption, especially for individuals with gastroduodenal disorders.

Innovation Solution

The formation of a FeII-ascorbate-proteinate complex in an aqueous medium at a pH of 4.8-6.8, using a solid or liquid oral composition containing ferrous salts, vitamin E, sodium ascorbate, and proteins, which promotes the absorption and maintenance of reduced iron while minimizing oxidative stress and side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If iron is administered in the form of salt (iron sulphate, iron fumarate, iron pyrophosphate), then iron supplementation is achieved, but gastric damage and side effects occur

Engineering Contradiction:
Improveiron supplementationVSAvoidgastric damage
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses magnesium oxide as an intermediary substance that reacts with gastric acid to form magnesium chloride, thereby neutralizing the harmful acidic environment that causes gastric damage from iron salts. This mediator protects the gastric mucosa while allowing iron absorption to proceed.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the pH parameter of the gastric environment by introducing magnesium oxide, which increases pH from highly acidic conditions to a less acidic state (pH 4.8-6.8), reducing the harmful effects on gastric tissue while maintaining conditions favorable for iron absorption.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If ferrous iron is used for absorption, then bioavailability is improved, but oxidation to ferric iron occurs in the presence of atmospheric oxygen and gastric fluids

Engineering Contradiction:
Improveiron bioavailabilityVSAvoidoxidation resistance
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

Vitamin E is introduced as a preliminary protective agent that prevents oxidation of ferrous iron before it can occur. The antioxidant acts in advance to neutralize oxidative processes initiated by atmospheric oxygen and gastric fluids, preserving the bioavailable ferrous state.

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The patent converts the harmful oxidative environment of the stomach into a beneficial condition by using vitamin E to scavenge free radicals and prevent oxidation, thereby transforming the potentially damaging oxidative atmosphere into a protective environment for ferrous iron.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Quantity of substance

If iron supplements are taken, then iron deficiency is treated, but unpleasant taste persists over time

Engineering Contradiction:
Improveiron treatment efficacyVSAvoidtaste acceptability
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

Magnesium oxide serves as a taste-modifying intermediary that not only protects against gastric damage but also improves the organoleptic properties of the formulation, masking the unpleasant metallic taste of iron salts while maintaining therapeutic efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 FeII-ascorbate-proteinate complex enhances iron bioavailability, reduces side effects, and improves absorption, particularly in the duodenal environment, maintaining reduced iron form and reducing oxidative stress, thus addressing the limitations of existing treatments.

Implementation Method 1

The mechanism of action of magnesium oxide consists in increasing the pH of the stomach to a less acidic state

Methodology Applied
Scientific EffectpH adjustment:

Implementation Method 2

The mechanism of action of vitamin E is based on its ability to prevent oxidation

Methodology Applied
Scientific EffectAntioxidant action: Oxidation

Implementation Method 3

The formation of a FeII-ascorbate-proteinate complex in an aqueous medium at a pH of 4.8-6.8

Methodology Applied
Scientific EffectComplex formation: Chemical Bonding

Implementation Method 4

promotes the absorption and maintenance of reduced iron while minimizing oxidative stress and side effects

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentEP3609473B1Oral compositions for the treatment of iron deficiency disorders
Publication Date: 2024.01.10 LABOMAR
  • EP3609473B1 patent drawingFigure 1
  • EP3609473B1 patent drawingFigure 2
  • EP3609473B1 patent drawingFigure 2A

AI summary

Aqueous medium having a pH between 4.8 and 6.8 and comprising the Fell- ascorbate-proteinate complex, prepared according to one of the following two alternative methods: (1) by dissolving in aqueous medium a solid oral composition (A) comprising an organic or inorganic ferrous salt, vitamin E, sodium ascorbate, plant or animal proteins and magnesium oxide in combination with suitable excipients and/or diluents, or (2) by forming a liquid oral composition (B) comprising the same components of the formulation (A) in combination with suitable excipients and/or diluents and water. Both the solid composition (A) in the method (1) and the liquid composition (B) in the method (2) are oral and are intended for the treatment of disorders and diseases caused by iron deficiency. A further object of the present invention relates to the preparation processes of the aforesaid solid composition (A) and liquid composition (B).