Iron (III) Casein Complex via N-Acetyl-L-Aspartyl Modification

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current iron therapy methods, especially parenteral routes, pose risks of allergic reactions and are costly, while oral iron therapies may not ensure optimal bioavailability and stability, particularly in treating iron deficiency conditions.

Innovation Solution

A process for preparing an iron (III) complex with N-acetyl-L-aspartylated casein, involving the reaction of casein with N-acetyl-L-aspartyl chloride and subsequent reaction with ferric chloride, resulting in a stable and bioavailable iron complex suitable for oral administration, using food-grade casein to ensure purity and safety.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If parenteral iron therapy is used, then iron deficiency can be treated effectively, but risks of serious allergic reactions and high cost increase

Engineering Contradiction:
Improveeffectiveness of iron deficiency treatmentVSAvoidallergic reactions and cost
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of casein by introducing N-acetyl-L-aspartyl groups through reaction with N-acetyl-L-aspartyl chloride. This chemical modification changes the parameters of the protein, creating new complexation sites for iron that improve bioavailability while enabling safe oral administration, thus avoiding the harmful effects of parenteral therapy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite material consisting of iron (III) ions complexed with modified casein protein chains. The composite structure combines the stability of iron complexes with the biocompatibility and solubility enhancement provided by the succinylated and N-acetyl-L-aspartylated casein, achieving both effectiveness and safety

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If oral iron therapy is used, then cost is reduced and allergic reaction risks are lowered, but bioavailability and stability may not be optimal

Engineering Contradiction:
Improvecost and allergic reaction risksVSAvoidbioavailability and stability
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent performs preliminary chemical modifications on casein before iron complexation. The casein is first succinylated to introduce carboxyl groups, then N-acetyl-L-aspartylated to create additional complexation sites. These preliminary actions enhance the protein's ability to complex iron, ensuring optimal bioavailability and stability for oral administration

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The chemical modification of casein changes key parameters including the number of available complexation sites, solubility characteristics, and stability profile. These parameter changes enable the iron complex to maintain stability in the gastrointestinal environment while achieving high bioavailability

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If casein is succinylated before iron complexation, then solubility and stability are improved, but additional manufacturing steps are required

Engineering Contradiction:
Improvesolubility and stability of iron complexVSAvoidnumber of manufacturing steps
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The succinylation of casein is performed as a preliminary step before iron complexation. This advance preparation introduces carboxyl groups that are essential for stable iron binding and improved solubility. By performing this modification beforehand, the subsequent iron complexation step can proceed more effectively

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent combines multiple modification steps (succinylation and N-acetyl-L-aspartylation) into a integrated process sequence. While multiple chemical transformations are performed, they are combined in a systematic manner that achieves the desired stability and solubility improvements through the synergistic effect of both modifications

Inventive Principle:
Principle #5Merging (Combining)

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 resulting iron (III) complex is highly stable, bioavailable, and safe for oral use, effectively addressing iron deficiency without the risks associated with parenteral therapies and ensuring maximum iron absorption in the intestinal tract.

Implementation Method 1

reaction of casein with N-acetyl-L-aspartyl chloride, to form N-acetyl-L-aspartylated casein

Methodology Applied
Scientific EffectChemical Bonding: Chemical Bonding

Implementation Method 2

subsequent reaction of the N-acetyl-L-aspartylated casein with ferric chloride; complexation of the iron

Methodology Applied
Scientific EffectChemical Bonding: Chemical Bonding

Data Source

PatentEP3034512B1A process for producing iron (III) casein N-acetyl-aspartylated complexes and use thereof in pharmaceutical compositions
Publication Date: 2017.12.06 TSETI IOULIA

AI summary

The present invention generally relates to new process for the preparation of iron (III) casein N-acetyl-aspartylated complexes. The product obtainable according to the method of the present invention may be safely used to the general population or animals in the therapy of iron deficiency. The process of the invention includes the steps of: (a) reaction of casein with N-acetyl-L-aspartyl chloride, to form N-acetyl-L-aspartylated casein, (b) subsequent reaction of the N-acetyl-L-aspartylated casein with ferric chloride; and (c) obtaining the iron (III) complex with N-acetyl-L-aspartylated casein.