There are two prerequisites for the therapeutic action of a drug, i.e., having sufficient bioavailability to and biopersistence at the locus of action after dosing and having intrinsic ability to produce desired pharmacodynamic effects in their major exposure forms, unchanged and metabolized. As a special branch of pharmacology of Chinese herbal medicines, pharmacokinetics is to investigate issues related to the medicines' efficacy and safety by assessing the herbal ingredients' bioavailability to and biopersistence at the locus of action in the body. Chinese herbal medicines are often herb combinations of complex mixture and contain multiple bioactive ingredients working in concert. Unlike most investigational synthetic drugs developed from bench to bedside, Chinese herbal medicines are often developed from bedside to bench to bedside. Accordingly, pharmacokinetic research on Chinese herbal medicines could serve as a crucial step in identifying the chemical basis of the medicines' therapeutic actions and could facilitate development of new herbal medicines with enhanced efficacy and safety by using the right herbal ingredients in the right way. Mainly based on studies by the author's research group, this article illustrates approach to and methodology of multi-compound pharmacokinetic research on Chinese herbal medicines.