The discrimination and evaluation of stereoselective metabolism of enantiomers are of paramount significance for developing effective and safe chiral drugs. However, there is still a lack of comprehensive and in-depth understanding of stereospecific disposition of chiral components in Herbal Medicines. In this article, stereoselective methods including capillary electrophoresis, high-performance liquid chromatography, gas chromatography, supercritical fluid chromatography and hyphenation techniques for chiral drug metabolism studies are reviewed. Furthermore, applications of modern analytical techniques to study enantioselective metabolic profiling of the active components from Herbal Medicines in vitro and in vivo in recent years are also presented and the representative examples are enumerated.
Keywords: Chiral analysis, Drug metabolism, Pharmacokinetics, Herbal medicines
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