Lanifibranor Form Beta Crystallization for Stable Scalable Manufacturing
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for non-alcoholic steatohepatitis (NASH) lack an approved therapy, and existing crystalline forms of lanifibranor suffer from instability and poor manufacturing scalability.
Innovation Solution
A stable crystalline form of lanifibranor (form beta) is developed, characterized by PXRD, DSC, TGA, and DVS, prepared through a method involving heating in acetic acid and slow cooling, which enhances crystallinity, purity, and stability, allowing scalable production.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If existing crystalline forms of lanifibranor are used, then the compound can be obtained, but the crystallinity and stability are insufficient
Solution Approach 1:
The patent applies parameter changes by modifying the crystallization conditions, specifically using acetic acid as a solvent and controlling the cooling rate from heated solution to room temperature. This changes the physical parameters of the crystallization process to produce form beta with superior crystallinity and stability compared to previously known forms.
Solution Approach 2:
The invention utilizes phase transitions by heating the lanifibranor solution in acetic acid and then slowly cooling it to room temperature. This controlled phase transition from dissolved state to crystalline state enables the formation of the stable form beta crystal structure with defined PXRD patterns and favorable mechanical properties.
2Productivity
If lanifibranor is prepared without specific crystallization control, then production can proceed, but scalability and purity are limited
Solution Approach 1:
The patent applies preliminary action by pre-heating the lanifibranor solution in acetic acid before controlled cooling. This preliminary heating step ensures complete dissolution and uniform distribution of the compound in the solvent, which facilitates subsequent scalable production while maintaining high purity and consistent crystalline form beta formation.
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 crystalline form beta of lanifibranor exhibits high crystallinity, low hygroscopicity, favorable mechanical properties, and stability, enabling effective treatment of NASH and preventing progression from compensated to decompensated cirrhosis.
Implementation Method 1
heating a solution of lanifibranor in acetic acid and slowly cooling the resulting solution to room temperature
Data Source
AI summary
The present invention relates to a crystalline form of lanifibranor having an X-ray diffraction pattern in accordance with FIG. 1.