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Influence of Verapamil on Pharmacokinetics of Triptolide in Rats

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Abstract

The aim of this study was to investigate the role of P-glycoprotein (P-gp) in the intestinal absorption of triptolide. In this research, the bidirectional transport of triptolide across Caco-2 cells was studied in vitro. Moreover, the pharmacokinetic profiles of orally administered triptolide with and without pretreatment with verapamil were determined in rats. A markedly higher transport of triptolide across Caco-2 cells was observed in the basolateral-to-apical direction and was abrogated in the presence of the P-gp inhibitor, verapamil. The result indicated that P-gp might be involved in the absorption of triptolide. When the rats were pretreated with verapamil, the C max of triptolide increased from 423.01 ± 19.59 to 565.33 ± 20.27 ng/mL (33.6 %), and the AUC0–6 h increased by approximately 57 % when co-administered with verapamil. It was demonstrated that P-gp was involved in the transport of triptolide, which might exhibit a role in limiting its absorption and attenuating the toxicity of triptolide.

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Conflict of interest

The authors report no conflict of interest.

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Authors and Affiliations

  1. Department of Hepato-Biliary Surgery, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China

    Yichuan Zhang, Jin Li & Maohui Yang

  2. Department of Oncology, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China

    Xiaolin Lei

  3. Department of Traditional Medicine, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China

    Tianying Zhang

  4. Department of Pharmacy, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China

    Guangxian Liu

  5. Department of Rheumatology, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China

    Min Liu

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  1. Yichuan Zhang
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  2. Jin Li
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  3. Xiaolin Lei
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  4. Tianying Zhang
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  5. Guangxian Liu
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  7. Min Liu
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Correspondence to Min Liu.

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Zhang, Y., Li, J., Lei, X. et al. Influence of Verapamil on Pharmacokinetics of Triptolide in Rats. Eur J Drug Metab Pharmacokinet 41, 449–456 (2016). https://doi.org/10.1007/s13318-015-0275-4

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  • DOI: https://doi.org/10.1007/s13318-015-0275-4

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