Elafibranor Crystalline Forms for Stability and Solubility

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Solution Overview

Problem

Existing polymorphic forms of elafibranor do not provide optimal physicochemical properties, affecting shelf life, solubility, and formulation properties, necessitating the development of improved crystalline forms for pharmaceutical applications.

Innovation Solution

Identification and characterization of five new crystalline forms of elafibranor, including forms B, C, D, and E, which offer improved chemical purity, flowability, solubility, and stability, suitable for pharmaceutical compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the existing polymorphic form of elafibranor is used, then the manufacturing process is simple, but the shelf life and solubility are not optimal

Engineering Contradiction:

Improveshelf lifeVSAvoidmanufacturing complexity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by identifying and characterizing five distinct crystalline forms (A, B, C, D, and E) of elafibranor, each with unique X-ray diffraction patterns and physicochemical properties. This allows selection of the optimal polymorphic form based on desired properties such as shelf life, solubility, and stability, while maintaining a straightforward crystallization process from solvent solutions.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If the existing polymorphic form of elafibranor is used, then the formulation process is straightforward, but the solubility and flowability are insufficient

Engineering Contradiction:

ImprovesolubilityVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent resolves this contradiction by providing multiple crystalline forms with different solubility and flowability characteristics. Each form is characterized by specific X-ray diffraction patterns, allowing formulators to select the appropriate polymorph for their specific application requirements without increasing formulation complexity.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If the existing polymorphic form of elafibranor is used, then the processing is simple, but the chemical purity and stability are not optimal

Engineering Contradiction:

Improvechemical purityVSAvoidprocessing efficiency

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent addresses this contradiction by identifying five distinct crystalline forms with varying purity and stability profiles. The characterization methods including X-ray diffraction, DSC, and TGA enable rapid identification and selection of the optimal form, maintaining processing efficiency while achieving superior chemical purity and stability.

Inventive Principle:

Principle #35Parameter changes

4Adaptability or versatility

If a single crystalline form is used, then the manufacturing is simple, but the adaptability to different pharmaceutical applications is limited

Engineering Contradiction:

Improveapplication versatilityVSAvoidpolymorph selection

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent resolves this contradiction by providing five distinct crystalline forms (A, B, C, D, and E), each with unique physicochemical properties and X-ray diffraction patterns. This diversity enables adaptation to various pharmaceutical applications including different dosage forms, routes of administration, and storage conditions, while the clear characterization methods simplify the selection process.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12522564B2Polymorphs of elafibranor

Publication Date: 2026.01.13 GENFIT SA

AI summary

The present invention relates to novel crystalline forms of elafibranor.