The Role of Liquid Chromatography-Mass Spectrometry in Pharmacokinetics and Drug Metabolism

THE ROLE OF LIQUID CHROMATOGRAPHY-MASS SPECTROMETRY IN PHARMACOKINETICS AND DRUG METABOLISM 

Recent advances in mass spectrometry have rendered it an attractive and versatile tool in industrial and academic research laboratories. As a part of this rapid growth, a considerable body of hterature has been devoted to the apph-cation of mass spectrometry in clinical studies. In concert with separation techniques such as hquid chromatography, mass spectrometry allows the rapid characterization and quantitative determination of a large array of molecules in complex mixtures. Herein, we present an overview of the above techniques accompanied with several examples of the use of liquid chromatography-tandem mass spectrometry in pharmacokinetics/drug metabohsm assessment during drug development. 

Since the evolution of pharmaceutical research [1,2], the stages of drug discovery and development have followed three predominant patterns (i) the systematic and methodical approach by chemists to rationally design and synthesize a molecule to target a specific molecular system (e.g., ion channels, receptors, enzymes, DNA) (ii) the isolation and purification of the active ingredients of medicinal plants or microorganisms to screen their spectrum of 

HPLC for Pharmaceutical Scientists, Edited by Yuri Kazakevich and Rosario LoBrutto Copyright 2007 by John Wiley Sons, Inc. 

Furthermore, samples generated from large-scale clinical trials along with the ambitious development timelines to get safe and efficacious drugs to market warrant the use of HT bioanalysis. Numerous improvements in speed, sensitivity, and accuracy, augmented with innovations in automation in conjunction with mass spectrometry (MS) detection, have allowed for versatile and multifaceted platforms [6-8]. 

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