Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
iDDPartners, 3 Edith Court
Princeton Junction
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Fast Mass Spectrometry-Based Methodologies for Pharmaceutical Analyses

Author(s): Yunsheng Hsieh, Elaine Fukuda, Julie Wingate, Walter A. Korfmacher.


Historically, most bioanalytical methods for drug analysis in pharmaceutical industry were developed using HPLC coupled with UV or fluorescence detection. However, there is a trend toward interfacing separation technologies with more sensitive tandem mass spectrometry (MS/MS)-based systems. MS/MS detection offers complete resolution of the parent compounds from their first pass metabolites to avoid extra efforts for separation and sample clean-up procedures resulting in shorter run times. With the increasing demand for ever faster screening, there is a continuing demand for bioanalytical methods possessing higher sample throughput for both in vitro and in vivo drug metabolism and pharmacokinetic evaluations to accelerate the discovery process. This review focuses on the current approaches for fast MS-based assays (cycle-time less than 5 min) of pharmaceuticals and their metabolites that have been reported in the peer-reviewed publications.

Keywords: chromatographic separation, ultra-performance liquid chromatography, atmospheric pressure chemical ionization (APCI), chiral stationary phases, quantitative analysis, bioassays

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Article Details

Year: 2006
Page: [3 - 8]
Pages: 6
DOI: 10.2174/138620706775213895