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Reduction of Punch-Sticking Propensity of Celecoxib by Spherical Crystallization via Polymer Assisted Quasi-Emulsion Solvent Diffusion.
Mol Pharm. 2020 04 06; 17(4):1387-1396.MP

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.

Authors+Show Affiliations

Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.Department of Chemical Engineering and Materials Science, University of Minnesota, Minneapolis, Minnesota 55455, United States.Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.Department of Chemical Engineering and Materials Science, University of Minnesota, Minneapolis, Minnesota 55455, United States.Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.

Language

eng

PubMed ID

32134675

Citation

Chen, Hongbo, et al. "Reduction of Punch-Sticking Propensity of Celecoxib By Spherical Crystallization Via Polymer Assisted Quasi-Emulsion Solvent Diffusion." Molecular Pharmaceutics, vol. 17, no. 4, 2020, pp. 1387-1396.
Chen H, Paul S, Xu H, et al. Reduction of Punch-Sticking Propensity of Celecoxib by Spherical Crystallization via Polymer Assisted Quasi-Emulsion Solvent Diffusion. Mol Pharm. 2020;17(4):1387-1396.
Chen, H., Paul, S., Xu, H., Wang, K., Mahanthappa, M. K., & Sun, C. C. (2020). Reduction of Punch-Sticking Propensity of Celecoxib by Spherical Crystallization via Polymer Assisted Quasi-Emulsion Solvent Diffusion. Molecular Pharmaceutics, 17(4), 1387-1396. https://doi.org/10.1021/acs.molpharmaceut.0c00086
Chen H, et al. Reduction of Punch-Sticking Propensity of Celecoxib By Spherical Crystallization Via Polymer Assisted Quasi-Emulsion Solvent Diffusion. Mol Pharm. 2020 04 6;17(4):1387-1396. PubMed PMID: 32134675.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Reduction of Punch-Sticking Propensity of Celecoxib by Spherical Crystallization via Polymer Assisted Quasi-Emulsion Solvent Diffusion. AU - Chen,Hongbo, AU - Paul,Shubhajit, AU - Xu,Hongyun, AU - Wang,Kunlin, AU - Mahanthappa,Mahesh K, AU - Sun,Changquan Calvin, Y1 - 2020/03/24/ PY - 2020/3/7/pubmed PY - 2021/5/29/medline PY - 2020/3/6/entrez KW - Celecoxib KW - HPMC KW - punch sticking KW - spherical crystallization KW - surface coating SP - 1387 EP - 1396 JF - Molecular pharmaceutics JO - Mol Pharm VL - 17 IS - 4 N2 - 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. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/32134675/Reduction_of_Punch_Sticking_Propensity_of_Celecoxib_by_Spherical_Crystallization_via_Polymer_Assisted_Quasi_Emulsion_Solvent_Diffusion_ L2 - https://doi.org/10.1021/acs.molpharmaceut.0c00086 DB - PRIME DP - Unbound Medicine ER -