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Pharmacokinetic Profiling of Butylidenephthalide and Alisol B in Danggui-Shaoyao-San in Rats

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European Journal of Drug Metabolism and Pharmacokinetics Aims and scope Submit manuscript

Abstract

Background and Objective

Danggui-Shaoyao-San (DSS), a famous Chinese formula, has been widely used to treat gynecological disorders since ancient times and has recently showed efficacy in treating Alzheimer’s disease. Butylidenephthalide (BDPH) and alisol B (ALI) are recognized as the primary active ingredients of DSS. The objectives of the present study were to evaluate the pharmacokinetic comparative study of BDPH and ALI in herbal extracts and their purified forms.

Method

A sensitive and specific high-performance liquid chromatography tandem mass spectrometry (HPLC–MS/MS) methodology was developed to determine the concentration level of BDPH and ALI in rat plasma. This approach enables a real-time pharmacokinetics profiling of BDPH and ALI in DSS extracts as well as their purified forms in rats after oral administration.

Results

The validated method showed an evident linearity over a wide range of dosages (r > 0.99) with sensitivity down to 1.0 ng/mL for each analyte. The extraction recovery of the analyte ranged from 80.8 to 99.1%. The pharmacokinetic parameters were significantly different in herbal extracts and their purified forms. The results showed that the absorption of both BDPH and ALI from DSS extracts was significantly greater compared with their purified forms.

Conclusions

A highly specific, sensitive and rapid HPLC–MS/MS method was developed and applied for the determination of BDPH and ALI in rat plasma. It was found that BDPH and ALI had higher bioavailability in the DSS extract compared with their purified forms.

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Author information

Author notes

  1. Hui-fei Wu and Xiang-yu Wang contributed equally to this work and should be considered as co-first authors.

Authors and Affiliations

  1. Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, No. 12 Jichang Road, Guangzhou, 510405, Guangdong, China

    Hui-fei Wu, Xiang-yu Wang, Qi Wang & Wei-rong Li

  2. School of Chinese Meteria Medica, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China

    Hui-fei Wu & Shi-jian Quan

  3. Hospital of Traditional Chinese Medicine of Zhongshan, Zhongshan, 528400, China

    Hui-fei Wu

  4. School of Bioscience and Bioengineering, South China University of Technology, Guangzhou, 510640, China

    Ji-feng Deng

Authors
  1. Hui-fei Wu
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  2. Xiang-yu Wang
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  4. Shi-jian Quan
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  5. Qi Wang
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Corresponding authors

Correspondence to Qi Wang or Wei-rong Li.

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Funding

This work was supported by the National Natural Science Foundation of China (nos. 81473740, 81573638, 81673627, 81674040), the Natural Science Foundation of Guangdong Province (no. 2017A030313666) and Guangzhou Science Technology and Innovation Commission Technology Research Projects (no. 201805010005).

Conflict of interest

Hui-fei Wu, Xiang-yu Wang, Ji-feng Deng, Shi-jian Quan, Qi Wang and Wei-rong Li declare that they have no conflict of interest.

Ethical approval

The experimental design was approved by the Guangzhou University of Chinese Medicine Committee on Animal Care and Use, and the study was performed in accordance with the Internal Charter on the Humane Care and Use of Laboratory Animals.

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Wu, Hf., Wang, Xy., Deng, Jf. et al. Pharmacokinetic Profiling of Butylidenephthalide and Alisol B in Danggui-Shaoyao-San in Rats. Eur J Drug Metab Pharmacokinet 43, 645–653 (2018). https://doi.org/10.1007/s13318-018-0476-8

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  • DOI: https://doi.org/10.1007/s13318-018-0476-8

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