Perampanel Anhydrous Crystalline Forms for Stability
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Solution Overview
Problem
There is a need for solid state forms of perampanel with good physicochemical properties and desirable bioavailability for effective pharmaceutical use in treating epilepsy and seizures, as existing forms may lack stability and optimal bioavailability.
Innovation Solution
The development of novel anhydrous crystalline forms of perampanel, specifically Forms III, V, and VII, characterized by unique X-ray diffraction patterns and thermal profiles, which are prepared through specific solvent mixtures and evaporation processes, enhancing their stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing crystalline forms of perampanel are used, then the basic pharmaceutical function is achieved, but stability and bioavailability are insufficient
Solution Approach 1:
The patent applies parameter changes by discovering and utilizing different crystalline polymorphic forms (Forms I, III, V, and VII) of perampanel, each with distinct X-ray diffraction patterns and physical properties. By changing the crystalline structure parameters through specific synthesis methods and solvent systems, the invention achieves improved stability and bioavailability compared to previously known forms.
Solution Approach 2:
The patent creates composite pharmaceutical compositions by combining perampanel in specific crystalline forms with pharmaceutically acceptable carriers and excipients. These composite materials optimize both stability and bioavailability, resolving the contradiction between the two properties through careful formulation design.
2Ease of manufacture
If perampanel is synthesized using conventional methods, then the chemical structure is obtained, but the polymorphic nature and physical properties are not optimized
Solution Approach 1:
The patent applies preliminary action by establishing specific synthesis protocols and purification procedures that pre-determine the formation of desired polymorphic forms. By controlling crystallization conditions, solvent systems, and processing parameters in advance, the invention ensures consistent production of stable polymorphic forms with optimized properties.
3Device complexity
If perampanel is formulated without optimizing crystalline form, then formulation development is simplified, but dissolution rate and bioavailability are compromised
Solution Approach 1:
The patent resolves this contradiction by changing the crystalline form parameters to achieve Forms I, III, V, and VII, which exhibit improved dissolution rates and bioavailability. While this requires specific synthesis and characterization methods, the resulting formulations demonstrate enhanced performance that justifies the additional complexity.
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
These new forms exhibit improved stability, bioavailability, and solubility, making them suitable for various pharmaceutical formulations and effective in treating epilepsy and seizures, particularly partial-onset seizures with or without secondarily generalized seizures.
Implementation Method 1
which are prepared through specific solvent mixtures and evaporation processes
Implementation Method 2
The development of novel anhydrous crystalline forms of perampanel, specifically Forms III, V, and VII, characterized by unique X-ray diffraction patterns
Data Source
AI summary
The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.