Small-Molecule Povidone Analogues in Coamorphous Pharmaceutical Phases

摘要

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).