Reduction of Punch-Sticking Propensity of Celecoxib by Spherical Crystallization via Polymer Assisted Quasi-Emulsion Solvent Diffusion.

Molecular Pharmaceutics
Hongbo ChenChangquan Calvin Sun

Abstract

Punch-sticking during tablet compression is a common problem for many active pharmaceutical ingredients (APIs), which renders tablet formulation development challenging. Herein, we demonstrate that the punch-sticking propensity of a highly sticky API, celecoxib (CEL), can be effectively reduced by spherical crystallization enabled by a polymer assisted quasi-emulsion solvent diffusion (QESD) process. Among three commonly used pharmaceutical polymers, poly(vinylpyrrolidone) (PVP), hydroxypropyl cellulose (HPC), and hydroxypropyl methylcellulose (HPMC), HPMC was the most effective in stabilizing the transient emulsion during QESD and retarding the coalescence of emulsion droplets and the initiation of CEL crystallization. These observations may arise from stronger intermolecular interactions between HPMC and CEL, consistent with solution 1H NMR analyses. SEM and X-ray photoelectron spectroscopy confirmed the presence of a thin layer of HPMC on the surfaces of spherical particles. Thus, the sticking propensity was significantly reduced because the HPMC coating prevents direct contact between CEL and the punch tip during tablet compression.

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Feb 25, 2017·International Journal of Pharmaceutics·Shubhajit PaulChangquan Calvin Sun
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Nov 19, 2018·Journal of Pharmaceutical Sciences·Hongbo ChenChangquan Calvin Sun
Nov 30, 2018·Molecular Pharmaceutics·Milankumar S JasaniArvind K Bansal

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Citations

Jul 7, 2020·Acta Crystallographica. Section C, Structural Chemistry·Andrew D Bond, Changquan C Sun
Jan 19, 2021·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Jerome Hansen, Peter Kleinebudde
Jan 24, 2021·International Journal of Pharmaceutics·Kunlin Wang, Changquan Calvin Sun
Jun 14, 2021·International Journal of Pharmaceutics·Jerome Hansen, Peter Kleinebudde

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