Small-Molecule Povidone Analogues in Coamorphous Pharmaceutical Phases

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, carbarnazepine, isoniazid, and 5-methyl-2-[(2-nitrophenyl)amino]-3-thiophenecarbonitrile (ROY).