Background: Botanical drugs contain plant extracts, which are complex mixtures of compounds.
As with conventional drugs, it is necessary to validate their efficacy and safety through preclinical
and clinical studies. However, pharmacokinetic studies for active constituents or characteristic
markers in botanical drugs are rare.
Objective: The objective of this review was to investigate the global state of the art in pharmacokinetic
studies of active ingredients present in plant extracts and botanical drugs. A review of pharmacokinetics
studies of chemical constituents of plant extracts and botanical drugs was performed, with a total of
135 studies published between January 2004 and February 2015 available in recognized scientific databases.
Botanical preparations were mainly found in the form of aqueous extracts of roots and rhizomes.
The most widely studied species was Salvia miltiorrhiza Bunge, and the compound most frequently
used as a pharmacokinetic marker was berberine.
Conclusion: Most studies were performed using the Sprague Dawley rat model, and the preparations
were mainly administered orally in a single dose. Quantification of plasma concentrations of pharmacokinetic
markers was performed mainly by liquid-liquid extraction, followed by high performance liquid
chromatography coupled to mass spectrometry detector. In conclusion, in recent years there has been an
increasing interest among researchers worldwide in the study of pharmacokinetics of bioactive compounds
in botanical drugs and plant extracts, especially those from the Traditional Chinese Medicine.