Ferroporphyrin Solid Dispersion via Cyclodextrin Inclusion

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Solution Overview

Problem

Current iron supplement agents, such as ferrous sulfate and ferroporphyrin, suffer from issues like poor bioavailability, gastrointestinal irritation, and instability, leading to low compliance and effectiveness in treating iron deficiency anemia, with existing formulations failing to adequately address these issues.

Innovation Solution

A porphyrin iron solid dispersion is created using a carrier material like polymers with vinylpyrrolidone units or celluloses, where porphyrin iron is dispersed at a molecular level through a hot melt extrusion process, improving bioavailability, stability, and mouthfeel while reducing gastrointestinal irritation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If porphyrin iron is used as an iron supplement, then iron supplementing effect is improved, but water solubility deteriorates

Engineering Contradiction:

Improveiron supplementing effectVSAvoidwater solubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the physical state and solubility parameters of porphyrin iron by forming a solid dispersion with cyclodextrin inclusion complexes. This transforms the insoluble porphyrin iron into a water-soluble complex, resolving the contradiction between maintaining iron supplementing effect and improving water solubility.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite material system consisting of porphyrin iron, cyclodextrin, and auxiliary ingredients. The cyclodextrin acts as a carrier that forms inclusion complexes with porphyrin iron, creating a composite that combines the iron supplementing properties of porphyrin iron with the water solubility of cyclodextrin.

Inventive Principle:

Principle #40Composite materials

2Reliability

If porphyrin iron is used as an iron supplement, then iron supplementing effect is improved, but stability deteriorates

Engineering Contradiction:

Improveiron supplementing effectVSAvoidoxidation stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent introduces cyclodextrin as an intermediary substance that forms inclusion complexes with porphyrin iron. This intermediary protects the ferrous iron from oxidation by isolating it from environmental factors, thereby maintaining both the iron supplementing effect and oxidation stability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The cyclodextrin inclusion complex creates a protected microenvironment around the porphyrin iron, effectively creating an inert atmosphere that prevents oxidation. This allows the iron supplement to maintain its stability while retaining its biological activity.

Inventive Principle:

Principle #39Inert atmosphere (Inert environment)

3Reliability

If porphyrin iron is used as an iron supplement, then iron supplementing effect is improved, but gastrointestinal irritation worsens

Engineering Contradiction:

Improveiron supplementing effectVSAvoidgastrointestinal irritation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The cyclodextrin acts as a mediator between the porphyrin iron and the gastrointestinal tract. It forms an inclusion complex that masks the irritating properties of porphyrin iron while allowing the iron to be released and absorbed in the intestine, thus reducing gastrointestinal irritation while maintaining iron supplementing effect.

Inventive Principle:

Principle #24Intermediary (Mediator)

4Reliability

If porphyrin iron is used as an iron supplement, then iron supplementing effect is improved, but taste worsens

Engineering Contradiction:

Improveiron supplementing effectVSAvoidblood smell and taste

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The cyclodextrin inclusion complex acts as a masking intermediary that encapsulates the porphyrin iron, hiding its characteristic blood smell and unpleasant taste. The complex allows the iron to be delivered to the intestine while preventing the sensory defects from being perceived by the patient.

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 porphyrin iron solid dispersion enhances bioavailability, stability, and patient compliance by masking the blood smell and reducing gastrointestinal irritation, with improved solubility and dissolution rates, making it a more effective iron supplement.

Implementation Method 1

porphyrin iron is dispersed at a molecular level through a hot melt extrusion process

Methodology Applied

Scientific EffectMolecular dispersion: Dispersion (of waves)

Implementation Method 2

dispersed at a molecular level through a hot melt extrusion process

Methodology Applied

Scientific EffectHeating: Heating

Data Source

PatentUS10391103B2Ferroporphyrin solid dispersion and preparation method thereof

Publication Date: 2019.08.27 SINOTHERAPEUTICS

AI summary

Disclosed are a ferroporphyrin solid dispersion, preparation method therefor and a pharmaceutical composition comprising the solid dispersion, wherein the weight ratio of ferroporphyrin to the carrier material in the dispersion is 1:1-1:10. The solid dispersion of the present invention masks the undesirable taste of ferroporphyrin, ameliorates irritation thereof to the digestive tract, and at the same time increases the solubility thereof and improves the bioavailability thereof.