Delayed Release Deferiprone Tablets for Reduced Gastric Distress

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Solution Overview

Problem

Existing immediate release deferiprone tablets cause gastric distress and require frequent dosing, leading to non-compliance due to discomfort, while extended release formulations compromise peak serum concentration and efficacy.

Innovation Solution

A delayed release tablet formulation with an enteric coating that allows twice daily dosing, maintaining bioequivalence to three times daily immediate release tablets, minimizing gastric distress, and achieving similar peak serum concentrations and absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If immediate release deferiprone tablets are administered three times daily, then therapeutic efficacy is maintained, but gastric distress and patient compliance deteriorate

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidgastric distress

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The tablet is divided into multiple dose units within a single scored tablet, allowing patients to take one tablet containing multiple doses or split tablets to reduce frequency of administration while maintaining total daily dose for therapeutic efficacy

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The enteric coating is applied in advance to protect the deferiprone from gastric acid degradation and irritation before administration, preventing gastric distress while maintaining drug availability for therapy

Inventive Principle:

Principle #10Preliminary action

2Reliability

If immediate release deferiprone tablets are administered three times daily, then therapeutic efficacy is maintained, but patient compliance deteriorates

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The formulation changes from immediate release to delayed release with enteric coating, altering the release parameters to extend duration of action and reduce dosing frequency while maintaining efficacy

Inventive Principle:

Principle #35Parameter changes

3Ease of operation

If extended release formulations are used, then dosing frequency is reduced, but peak serum concentration and efficacy deteriorate

Engineering Contradiction:

Improvedosing frequencyVSAvoidpeak serum concentration

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The formulation uses enteric coating to change the release parameters, delaying release until the drug reaches the intestine where it is then released rapidly, achieving both reduced dosing frequency and maintained peak concentrations

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The enteric coating acts as an intermediary layer that controls the release timing, protecting the drug from premature release in the stomach while ensuring rapid release in the intestine to maintain peak serum concentrations

Inventive Principle:

Principle #24Intermediary (Mediator)

4Ease of operation

If delayed release tablet is administered twice daily, then patient compliance improves, but bioequivalence to three times daily immediate release must be maintained

Engineering Contradiction:

Improvepatient complianceVSAvoidbioequivalence

Core Design Contradiction:

Ease of operationVSManufacturing precision

Solution Approach 1:

The formulation parameters including enteric coating thickness, core composition, and scoring are precisely controlled to ensure that twice daily administration of the delayed release tablet achieves the same area under the curve and peak concentrations as three times daily immediate release

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 delayed release tablets provide effective iron chelation therapy with reduced gastric discomfort and improved patient compliance by maintaining therapeutic efficacy with twice daily administration.

Implementation Method 1

a delayed release tablet comprising deferiprone for oral administration to a human subject, wherein twice daily administration of the delayed release tablet is bioequivalent in the steady state to the same daily dose of an immediate release tablet comprising deferiprone administered three times daily

Methodology Applied

Scientific EffectEnteric coating delayed release: Physical Containment

Data Source

PatentEP3684344B1Delayed release deferiprone tablets and methods of using the same

Publication Date: 2025.07.02 CHIESI FARMACEUTICI SPA

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AI summary

The invention is directed to pharmaceutical compositions such as tablets that exhibit delayed release properties when administered as either whole or half tablets. The invention is also directed to delayed release tablets comprising deferiprone for oral administration, for which twice daily administration is bioequivalent to the same daily dose of an immediate release tablet administered thrice daily. The invention is also directed to methods of making and using the same.