Trofinetide Crystalline Forms for Chemical and Storage Stability
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Solution Overview
Problem
There is a need for chemically stable solid forms of trofinetide for treating conditions such as Rett Syndrome, Fragile X Syndrome, and traumatic brain injury.
Innovation Solution
Development of crystalline polymorphic forms of trofinetide and trofinetide hydrate, characterized by specific PXRD patterns, Raman spectra, and other physicochemical properties, which are chemically stable and suitable for pharmaceutical compositions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If crystalline polymorphic forms of trofinetide are developed, then chemical stability is improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by developing specific crystalline polymorphic forms with defined physical and chemical parameters. By controlling crystallization conditions (temperature, solvent composition, pH, additives) and characterizing the resulting crystal structures through PXRD patterns and other analytical methods, the invention achieves enhanced chemical stability of trofinetide in solid form while providing reproducible manufacturing processes for each polymorphic form.
2Duration of action of stationary object
If specific crystalline forms with defined PXRD patterns are produced, then storage stability is improved, but production process complexity increases
Solution Approach 1:
The patent applies preliminary action by pre-establishing and characterizing multiple crystalline polymorphic forms with their specific PXRD patterns, solubility profiles, and stability characteristics before clinical use. This allows selection of the most suitable polymorphic form for long-term storage and formulation development, avoiding stability issues during storage and distribution while simplifying later manufacturing by working with pre-validated crystal forms.
Solution Approach 2:
The patent utilizes phase transitions by controlling the crystallization process to produce specific polymorphic forms of trofinetide. By manipulating crystallization conditions (solvent selection, temperature profiles, addition rates, seeding), the invention directs the formation of desired crystal phases with specific stability and solubility properties, enabling optimized storage forms while maintaining control over the production process.
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 forms provide enhanced chemical stability, enabling effective treatment of conditions like traumatic brain injury and neurodevelopmental disorders, with improved storage stability and formulation compatibility.
Implementation Method 1
Development of crystalline polymorphic forms of trofinetide and trofinetide hydrate, characterized by specific PXRD patterns, Raman spectra, and other physicochemical properties, which are chemically stable
Data Source
AI summary
This disclosure provides crystalline forms of trofinetide and trofinetide hydrate, pharmaceutical compositions comprising crystalline forms of trofinetide and trofinetide hydrate, methods of making crystalline forms of trofinetide or trofinetide hydrate, and methods of treating a disease, condition, or disorder in a subject comprising administering a composition comprising crystalline forms of trofinetide or trofinetide hydrate to the subject.