J147 Crystalline Form II Stability and Solubility
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Solution Overview
Problem
The development of polymorph forms of the neuroprotective agent 2,2,2-trifluoroacetic acid 1-(2,4-Dimethylphenyl)-2-[(3-methoxyphenyl)methylene] hydrazide (J147) is necessary to address issues related to its physicochemical properties, such as stability, solubility, and pharmacokinetics, which are critical for effective administration and treatment of neurodegenerative diseases.
Innovation Solution
The disclosure provides methods for obtaining crystalline Form II of J147 through recrystallization from specific solvent/anti-solvent mixtures, including the use of water as an anti-solvent, and characterizes this form using X-ray diffraction patterns and other analytical techniques, demonstrating its stability and distinct properties compared to Form I.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If crystalline Form I of J147 is used, then the compound can be obtained through standard synthesis, but it exhibits insufficient stability and solubility for effective pharmaceutical administration
Solution Approach 1:
The patent applies parameter changes by modifying the crystallization conditions (solvent type, temperature, pH) to transform J147 from Form I to Form II polymorph, which possesses superior stability and solubility characteristics while maintaining the same chemical composition
Solution Approach 2:
The patent utilizes phase transitions by inducing a polymorphic transformation from Form I to Form II through controlled crystallization processes, including solvent selection and temperature cycling, to achieve the desired stability and solubility profile
2Stability of the object's composition
If crystalline Form I of J147 is used, then the compound can be synthesized through conventional methods, but it displays inadequate solubility for effective drug delivery
Solution Approach 1:
The patent modifies crystallization parameters including solvent selection (using water or water/organic mixtures), temperature profiles, and pH control to induce formation of Form II polymorph with enhanced solubility while maintaining manufacturing feasibility
Solution Approach 2:
The patent introduces solvent/anti-solvent systems as intermediaries to control the crystallization process and induce formation of the desired Form II polymorph with improved solubility characteristics
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 II of J147 exhibits improved stability and solubility, potentially enhancing its therapeutic efficacy and manufacturing processes, making it a more suitable form for pharmaceutical applications.
Implementation Method 1
mixing the slurry to provide crystalline Form II
Implementation Method 2
having a powder X-ray diffraction pattern comprising peaks located at 13.37, 18.47, and 23.34+/â0.2 degrees 2-theta
Data Source
AI summary
Crystalline polymorph forms of neurotrophic agent 2,2,2-trifluoroacetic acid 1-(2,4-Dimethylphenyl)-2-[(3-methoxyphenyl)methylene]hydrazide (J147), and process for producing the crystalline polymorphic form are provided.