Elafibranor Salt Forms Enhance Photostability and Solubility
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Solution Overview
Problem
The physicochemical properties of elafibranor, such as stability and solubility, particularly photostability, need improvement for effective pharmaceutical applications, especially in treating liver diseases like NAFLD, NASH, and cirrhosis.
Innovation Solution
Converting the free acid form of elafibranor into various salts, including tromethamine, potassium, and sodium salts, which are synthesized and characterized for enhanced chemical purity, stability, and solubility, and formulated into pharmaceutical compositions for improved therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If elafibranor is used in free acid form, then the molecular structure is simple, but the stability and solubility are insufficient
Solution Approach 1:
The patent applies parameter changes by converting elafibranor from free acid form to various salt forms (sodium, potassium, calcium, magnesium salts). This chemical parameter transformation improves stability and solubility while maintaining the core molecular structure through systematic modification of the counterion component.
Solution Approach 2:
The invention creates composite salt forms by combining elafibranor with different metal cations. Each salt form represents a composite material where elafibranor anions are paired with specific cations (Na+, K+, Ca2+, Mg2+), providing tailored physicochemical properties for different pharmaceutical applications.
2Reliability
If elafibranor is used in free acid form, then the formulation is simple, but the solubility is poor
Solution Approach 1:
The patent systematically changes the chemical parameter of elafibranor by forming salts with different cations. This transformation directly addresses solubility limitations while the standardized salt formation process maintains manufacturing feasibility through established pharmaceutical methodologies.
3Stability of the object's composition
If elafibranor is used in free acid form, then the photostability is insufficient, but converting to salts adds synthesis steps
Solution Approach 1:
The patent employs parameter changes by transforming elafibranor into salt forms that exhibit enhanced photostability. The synthesis steps added are standard salt formation procedures that, while increasing process steps, provide significant improvements in photostability essential for pharmaceutical stability requirements.
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 salt forms of elafibranor exhibit improved stability, solubility, and purity, leading to enhanced therapeutic effectiveness in treating liver diseases like NAFLD, NASH, and cirrhosis, with specific salt forms showing significant photostability and bioavailability advantages.
Implementation Method 1
converting the free acid of elafibranor into a salt of elafibranor
Data Source
AI summary
The present invention relates to salts of elafibranor.