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Small-Molecule Povidone Analogues in Coamorphous Pharmaceutical Phases
Crystal Growth & Design ( IF 3.8 ) Pub Date : 2018-01-08 00:00:00 , DOI: 10.1021/acs.cgd.7b01062
Melissa J. Goodwin 1 , Osama M. Musa 2 , David J. Berry 3 , Jonathan W. Steed 1
Affiliation  

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).

中文翻译:

非晶态药物相中的小分子聚维酮类似物

结晶抑制剂聚乙烯吡咯烷酮(PVP)通常在难溶性药物的无定形聚合物分散体形成中用作稳定剂。在这项工作中,我们研究了使用一系列受PVP启发的小分子双(内酰胺)作为稳定形成无定形药物相的无定形药物相中的共形成剂。N-乙烯基(己内酰胺)(bisVCap,3)的二聚体是相对较低的甲霜灵,卡马西平,异烟肼和5-甲基-2-[((2-硝基苯基)氨基]- 3-噻吩甲腈(ROY)。
更新日期:2018-01-08
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