(T1030-09-59) Spray-Dried Amorphous Solid Dispersions of Celecoxib-PVPVA64-SBEβCD Ternary Complexes: Preparation, Flory Huggins Interaction Parameters and Dissolution Enhancements

Purpose: Use sulfobutyl ether β-cyclodextrin (Captisol®) in ASDs to improve CXB solubility and dissolution while mitigating crystallization during storage and dissolution.

Methods: Spray drying was used to prepare both CXB:SBE-β-CD binary systems and CXB:SBE-β-CD:PVPVA64 ternary ASDs. The solid-state properties and dissolution behavior were assessed using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), intrinsic dissolution testing, and tablet dissolution studies.

Results: Intrinsic dissolution rate (IDR) studies showed a 20- to 50-fold increase in normalized dissolution rates for CXB in SBE-β-CD containing systems.

Conclusion: Presence of SBE-β-CD helps prevent crystallization at the surface as well as increase the saturation concentration at the interface.

References: Grandelli et al., Journal of Inclusion Phenomena and Macrocyclic Chemistry 2012, 77 (1-4), 269-277

Acknowledgements: 1. Department of Pharmaceutical Chemistry, University of Kansas
2. Ligand Pharmaceuticals

Impact on Celecoxib glass transition temperature and melting point in Celecoxib: SBE-β-CD binary mixtures

Degree of complexation modulated by the percentage of SBE-β-CD present.

Stationary disk intrinsic dissolution experiments: 20-50 fold rate enhancements for SBE-β-CD containing solid dispersions