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.
Original language | English (US) |
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Article number | 123041 |
Journal | International journal of pharmaceutics |
Volume | 641 |
DOIs | |
State | Published - Jun 25 2023 |
Bibliographical note
Funding Information:We thank Kunlin Wang for providing the Raman data of amorphous celecoxib. CCS thanks the National Science Foundation for support through the Industry University Collaborative Research Center grant IIP-2137264, Center for Integrated Materials Science and Engineering for Pharmaceutical Products (CIMSEPP).
Publisher Copyright:
© 2023 Elsevier B.V.
Keywords
- Direct compression
- Dissolution rate
- Mesoporous carrier
- Powder flow
- Punch sticking
PubMed: MeSH publication types
- Journal Article