Small-Molecule Povidone Analogs in Coamorphous Pharmaceutical Phases

Goodwin, Melissa; Musa, Osama; Berry, David; Steed, Jonathan W.

Abstract

The crystallization inhibitor polyvinylpyrrolidone (PVP) is commonly used as a stabilizer in the formation of amorphous polymer dispersions of poorly soluble pharmaceuticals. In this work we examine the use of a range of PVP-inspired small-molecule bis(lactams) as coformers in the stabilization of amorphous pharmaceutical phases creating coamorphous materials. The dimer of N-vinyl(caprolactam) (bisVCap, 3) was found to be an effective coamorphous-former at relatively low loading for carisoprodol, carbamazepine, isoniazid, and 5-methyl-2-[(2-nitrophenyl)amino]-3-thiophenecarbonitrile (ROY).

Citation

Goodwin, M., Musa, O., Berry, D., & Steed, J. W. (2018). Small-Molecule Povidone Analogs in Coamorphous Pharmaceutical Phases. Crystal Growth and Design, 18(2), 701-709. https://doi.org/10.1021/acs.cgd.7b01062

• Journal Article Type: Article
• Acceptance Date: Dec 18, 2017
• Online Publication Date: Jan 4, 2018
• Publication Date: Feb 7, 2018
• Deposit Date: Jan 5, 2018
• Publicly Available Date: Jan 4, 2019
• Journal: Crystal Growth and Design
• Print ISSN: 1528-7483
• Electronic ISSN: 1528-7505
• Publisher: American Chemical Society
• Peer Reviewed: Peer Reviewed
• Volume: 18
• Issue: 2
• Pages: 701-709
• DOI: https://doi.org/10.1021/acs.cgd.7b01062
• Public URL: https://durham-repository.worktribe.com/output/1341633