Multi-compound pharmacokinetic research on Chinese herbal medicines: identifying potentially therapeutic compounds and characterizing their disposition and pharmacokinetics / 药学学报

Chinese traditional medicine has provided, since ancient times, a basis for health care and medicine to the Chinese nation and for China's national stability. Identification of the constituents responsible for therapeutic and undesired effects of Chinese herbal medicines is a type of key research facilitating the modernization of these medicines. For a complex Chinese herbal medicine, multi-compound pharmacokinetic research is a useful approach to identifying its constituents that are bioavailable (in their unchanged and/or metabolized forms) at loci responsible for the medicine's therapeutic action and to characterizing the compounds' disposition and pharmacokinetics related to the action. In addition, such pharmacokinetic research is also useful for identifying herbal compounds associated with the medicine's adverse effects and drug-drug interaction potential. Over the past decade, great advances have been achieved in the theory, methodology, associated techniques, and their application of such multi-compound pharmacokinetic research, which has become an emerging field in pharmacokinetics. In this perspective, we elaborate on the methodology, technical requirements, and key analytical techniques of multi-compound pharmacokinetic research on Chinese herbal medicines, describe research examples regarding investigation of pharmacokinetics and disposition of a class of bioactive herbal constituents (ginsenosides of Panax notoginseng root) and pharmacokinetics-based identification of potential therapeutic compounds from a dosed Chinese herbal medicine (LianhuaQingwen capsule), and discuss follow-up development for the multi-compound pharmacokinetic research.

Multi-compound pharmacokinetic research on Chinese herbal medicines: approach and methodology / 中国中药杂志

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.