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High throughput screening of active pharmaceutical ingredients by UPLC
Author(s) -
AlSayah Mohammad A.,
Rizos Panagiota,
Antonucci Vincent,
Wu Naijun
Publication year - 2008
Publication title -
journal of separation science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.72
H-Index - 102
eISSN - 1615-9314
pISSN - 1615-9306
DOI - 10.1002/jssc.200700594
Subject(s) - chromatography , high performance liquid chromatography , active ingredient , chemistry , particle size , column (typography) , stationary phase , selectivity , analytical chemistry (journal) , computer science , bioinformatics , telecommunications , biochemistry , frame (networking) , biology , catalysis
Ultra performance LC (UPLC) was evaluated as an efficient screening approach to facilitate method development for drug candidates. Three stationary phases were screened: C‐18, phenyl, and Shield RP 18 with column dimensions of 150 mm×2.1 mm, 1.7 μm, which should theoretically generate ˜35 000 plates or ˜175% of the typical column plate count of a conventional 250 mm×4.6 mm, 5 μm particle column. Thirteen different active pharmaceutical ingredients (APIs) were screened using this column set with a standardized mobile‐phase gradient. The UPLC method selectivity results were compared to those obtained for these compounds via methods developed through laborious trial and error screening experiments using numerous conventional HPLC mobile and stationary phases. Peak capacity was compared for columns packed with 5 μm particles and columns packed with 1.7 μm particles. The impurities screened by UPLC were confirmed by LC/MS. The results demonstrate that simple, high efficiency UPLC gradients are a feasible and productive alternative to more conventional multiparametric chromatographic screening approaches for many compounds in the early stages of drug development.