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Pharmacokinetics of Chinese medicines: strategies and perspectives
Yan, Ru1,2; Yang, Ying1; Chen, Yijia1
2018-05-02
Source PublicationCHINESE MEDICINE
ISSN1749-8546
Volume13
Abstract

The modernization and internationalization of Chinese medicines (CMs) are hampered by increasing concerns on the safety and the efficacy. Pharmacokinetic (PK) study is indispensable to establish concentration-activity/toxicity relationship and facilitate target identification and new drug discovery from CMs. To cope with tremendous challenges rooted from chemical complexity of CMs, the classic PK strategies have evolved rapidly from PK study focusing on marker/main drug components to PK-PD correlation study adopting metabolomics approaches to characterize associations between disposition of global drug-related components and host metabolic network shifts. However, the majority of PK studies of CMs have adopted the approaches tailored for western medicines and focused on the systemic exposures of drug-related components, most of which were found to be too low to account for the holistic benefits of CMs. With an area under concentration-time curve-or activity-weighted approach, integral PK attempts to understand the PK-PD relevance with the integrated PK profile of multiple co-existing structural analogs (prototyes/metabolites). Cellular PK-PD complements traditional PK-PD when drug targets localize inside the cells, instead of at the surface of cell membrane or extracellular space. Considering the validated clinical benefits of CMs, reverse pharmacology-based reverse PK strategy was proposed to facilitate target identification and new drug discovery. Recently, gut microbiota have demonstrated multifaceted roles in drug efficacy/toxicity. In traditional oral intake, the presystemic interactions of CMs with gut microbiota seem inevitable, which can contribute to the holistic benefits of CMs through biotransforming CMs components, acting as the peripheral target, and regulating host drug disposition. Hence, we propose a global PK-PD approach which includes the presystemic interaction of CMs with gut microbiota and combines omics with physiologically based pharmacokinetic modeling to offer a comprehensive understanding of the PK-PD relationship of CMs. Moreover, validated clinical benefits of CMs and poor translational potential of animal PK data urge more research efforts in human PK study.

KeywordChinese Medicines Pharmacokinetic Strategy Pharmacokinetics-pharmacodynamics Relevance Gut Microbiota Global Pharmacokinetics-pharmacodynamics
DOI10.1186/s13020-018-0183-z
URLView the original
Indexed BySCI
Language英语
WOS Research AreaIntegrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS SubjectIntegrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS IDWOS:000431354900001
PublisherBIOMED CENTRAL LTD
The Source to ArticleWOS
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorYan, Ru
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macao, China.
2.Zhuhai UM Science & Technology Research Institute, Zhuhai 519080, China.
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Yan, Ru,Yang, Ying,Chen, Yijia. Pharmacokinetics of Chinese medicines: strategies and perspectives[J]. CHINESE MEDICINE,2018,13.
APA Yan, Ru,Yang, Ying,&Chen, Yijia.(2018).Pharmacokinetics of Chinese medicines: strategies and perspectives.CHINESE MEDICINE,13.
MLA Yan, Ru,et al."Pharmacokinetics of Chinese medicines: strategies and perspectives".CHINESE MEDICINE 13(2018).
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