Abstract

Drugs of different chiralities, when present in chiral environments (e.g., human body), usually have different pharmacokinetics/pharmacodynamics and thus have different therapeutic values. For this reason, in 1992, the U.S. Food and Drug Administration issued guidelines requiring drug companies to investigate the pharmacologic properties of racemic drugs in each of their enantiomeric forms. As a result, chiral separation techniques are of great importance today and are performed on a routine basis in pharmaceutical and biotechnology industries. This chapter will provide an overview of the approaches to chiral separations and application of chromatographic techniques in chiral recognition. Separation by physical process, such as enantiomeric crystallization, is not within the scope of this chapter. A brief overview will be provided to introduce the development of techniques that laid the groundwork for chiral chromatography. Classic theoretical models and interaction mechanisms for chiral recognition will be outlined. The most popular chiral chromatographic techniques, that is, HPLC, GC, and SFC, will be discussed in terms of the chiral selectors, separation mechanisms, strengths, limitations, and applications.

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