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Characterization of solid-state forms of celecoxib
Garima Chawla1, Piyush Gupta, R Thilagavathi
1Department of Pharmaceutical Technology (Formulations), National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160 062, India.
Summary
This research explores different solid-state forms of celecoxib, a COX-2 inhibitor, including solvates and an amorphous form. Characterization confirmed unique properties and influences on drug behavior.
Area of Science:
- Pharmaceutical Sciences
- Solid-State Chemistry
Background:
- Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor.
- Understanding its solid-state forms is crucial for drug formulation and efficacy.
Purpose of the Study:
- To generate and characterize various solid-state forms of celecoxib.
- To investigate the influence of these forms on physicochemical properties and behavior.
Main Methods:
- Polymorphic screening using diverse solvents (DMA, DMF).
- Amorphous form generation via quench cooling.
- Characterization using thermal analysis (DSC, TGA, HSM), XRD, microscopy (polarized, SEM), FTIR, and elemental analysis.
- Solubility, van't Hoff, and molecular modeling studies.
Main Results:
- Identified 1:1 stoichiometric solvates with DMA and DMF.
- Generated an amorphous celecoxib form through melt quench cooling.
- Characterized distinct properties of each solid-state form.
- Investigated the impact of morphology on flow properties.
Conclusions:
- Multiple solid-state forms of celecoxib exist, including solvates and an amorphous form.
- These forms exhibit unique characteristics influencing drug behavior.
- Detailed characterization provides insights for pharmaceutical development.