Gefapixant Solid State Forms for Stability and Bioavailability
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Solution Overview
Problem
There is a need for additional solid state forms of Gefapixant, including crystalline polymorphs and salts, to improve processing properties, stability, and bioavailability for the treatment of chronic cough, asthma, interstitial cystitis, musculoskeletal pain, and sleep apnea syndrome.
Innovation Solution
The development of crystalline polymorphs, salts, and co-crystals of Gefapixant, along with processes for their preparation, which can be used to create pharmaceutical compositions for enhanced therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If additional solid state forms of Gefapixant are developed, then stability and bioavailability are improved, but device complexity increases
Solution Approach 1:
The patent applies parameter changes by developing multiple solid state forms (polymorphs, salts, co-crystals) of Gefapixant with different crystal structures and physical properties. Each form represents a change in the physical parameters of the compound, allowing optimization of stability, solubility, and bioavailability while maintaining the same active pharmaceutical ingredient.
Solution Approach 2:
The patent employs composite materials by creating co-crystal forms of Gefapixant combined with different counterions or molecules. These composite solid state forms integrate multiple components into a single crystalline structure, enabling improved stability and bioavailability properties that neither component alone would provide.
2Ease of operation
If additional solid state forms of Gefapixant are developed, then handling characteristics are improved, but manufacturing complexity increases
Solution Approach 1:
The patent utilizes parameter changes by systematically varying the crystal structure parameters of Gefapixant through different polymorphic forms and salt formulations. These parameter changes result in materials with improved handling characteristics such as flowability, compressibility, and particle morphology, while the manufacturing processes follow established pharmaceutical development methodologies.
Data Source
AI summary
The present disclosure encompasses solid state forms of Gefapixant, in embodiments crystalline polymorphs or salts or co-crystals of Gefapixant, processes for preparation thereof, and pharmaceutical compositions thereof.