Tavapadon Solid State Forms for Stability and Bioavailability
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Solution Overview
Problem
There is a need for new solid state forms of Tavapadon, including crystalline polymorphs, co-crystals, and salts, to improve processing properties, stability, and bioavailability for the treatment of Parkinson's disease.
Innovation Solution
The development of crystalline polymorphs, co-crystals, and salts of Tavapadon, along with processes for their preparation, to create pharmaceutical compositions that enhance stability, bioavailability, and processing characteristics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If new solid state forms (polymorphs, co-crystals, salts) of Tavapadon are developed, then stability and bioavailability are improved, but the complexity of the formulation process increases
Solution Approach 1:
The patent applies parameter changes by developing multiple solid state forms (polymorphs, co-crystals, salts) of Tavapadon with different physical and chemical parameters. Each form exhibits distinct properties such as solubility, stability, and bioavailability, allowing optimization of formulation performance through selection of appropriate solid state forms rather than modifying the entire formulation process
Solution Approach 2:
The patent employs composite materials by creating co-crystals of Tavapadon with co-formers, forming composite solid state structures that combine Tavapadon molecules with other molecular entities. These co-crystals provide improved stability and bioavailability while maintaining a manageable formulation process through well-defined crystalline structures
2Reliability
If new solid state forms of Tavapadon are developed, then bioavailability is improved, but the manufacturing complexity increases
Solution Approach 1:
The patent utilizes parameter changes by developing different solid state forms (polymorphs, co-crystals, salts) with optimized dissolution and absorption parameters. These forms exhibit improved bioavailability through enhanced solubility and dissolution rates, while the manufacturing process remains relatively simple by using established crystallization and purification techniques
Solution Approach 2:
The patent introduces co-formers as intermediary substances that form co-crystals with Tavapadon. These co-formers act as mediators to improve the bioavailability of Tavapadon by creating solid state forms with favorable dissolution properties, while the co-crystallization process uses standard pharmaceutical manufacturing techniques
3Ease of manufacture
If multiple solid state forms are discovered, then processing properties are improved, but the difficulty of purification increases
Solution Approach 1:
The patent applies parameter changes by developing solid state forms with distinct physical parameters such as crystal structure, melting point, and solubility. These parameter differences enable improved processing properties including flowability, compressibility, and dissolution, while also providing clear analytical fingerprints for purification monitoring and form identification
4Reliability
If solid state forms with different crystal structures are created, then dissolution profile is improved, but the measurement and characterization complexity increases
Solution Approach 1:
The patent utilizes parameter changes by creating solid state forms with different crystal structures that exhibit distinct dissolution profiles. Each polymorph, co-crystal, or salt form has characteristic dissolution behavior that can be optimized for specific therapeutic needs, while the crystal structures provide unique X-ray diffraction patterns and other analytical fingerprints for straightforward characterization and quality control
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 new solid state forms of Tavapadon offer improved stability, bioavailability, and processing characteristics, potentially leading to more effective treatments for Parkinson's disease.
Implementation Method 1
Polymorphism, the occurrence of different crystalline forms, is a property of some molecules and molecular complexes. A single molecule may give rise to a variety of polymorphs having distinct crystal structures and physical properties like melting point, thermal behaviors (e.g., measured by thermogravimetric analysis ('TGA'), or differential scanning calorimetry ('DSC')), X-ray diffraction (XRD) pattern, infrared absorption fingerprint, and solid state (13C) NMR spectrum.
Implementation Method 2
X-ray diffraction (XRD) pattern
Implementation Method 3
X-ray diffraction (XRD) pattern
Implementation Method 4
thermal behaviors (e.g., measured by thermogravimetric analysis ('TGA'))
Implementation Method 5
differential scanning calorimetry ('DSC')
Implementation Method 6
infrared absorption fingerprint
Implementation Method 7
solid state (13C) NMR spectrum
Data Source
AI summary
The present disclosure encompasses solid state forms of Tavapadon, processes for preparation thereof, and pharmaceutical compositions thereof.