Enabling direct compression tablet formulation of celecoxib by simultaneously eliminating punch sticking, improving manufacturability, and enhancing dissolution …

S Paul, Y Guo, C Wang, J Dun, CC Sun - International journal of …, 2023 - Elsevier
International journal of pharmaceutics, 2023Elsevier
The development of a high quality tablet of Celecoxib (CEL) is challenged by poor
dissolution, poor flowability, and high punch sticking propensity of CEL. In this work, we
demonstrate a particle engineering approach, by loading a solution of CEL in an organic
solvent into a mesoporous carrier to form a coprocessed composite, to enable the
development of tablet formulations up to 40%(w/w) of CEL loading with excellent flowability
and tabletability, negligible punch sticking propensity, and a 3-fold increase in in vitro …
Abstract
The development of a high quality tablet of Celecoxib (CEL) is challenged by poor dissolution, poor flowability, and high punch sticking propensity of CEL. In this work, we demonstrate a particle engineering approach, by loading a solution of CEL in an organic solvent into a mesoporous carrier to form a coprocessed composite, to enable the development of tablet formulations up to 40% (w/w) of CEL loading with excellent flowability and tabletability, negligible punch sticking propensity, and a 3-fold increase in in vitro dissolution compared to a standard formulation of crystalline CEL. CEL is amorphous in the drug-carrier composite and remained physically stable after 6 months under accelerated stability conditions when the CEL loading in the composite was ≤ 20% (w/w). However, crystallization of CEL to different extents from the composites was observed under the same stability condition when CEL loading was 30–50% (w/w). The success with CEL encourages broader exploration of this particle engineering approach in enabling direct compression tablet formulations for other challenging active pharmaceutical ingredients.
Elsevier
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