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    Article

    Liquiritin Enhancing Intestinal Absorption of Paeoniflorin in in situ Single‑pass Intestinal Perfusion and in vitro Caco‑2 Cell Monolayer Absorption Models

    Rui He2, Sihui Wang2, Qing Liu2, Kaili Xie2, Yongsong Xu2, Jinli Shi3, Zhimin Wang4, Muxin Gong1★★ Corresponding author

    1. 1Department of Pharmaceutics of TCM, Beijing Key Lab of TCM Collateral Disease Theory Research, School of Traditional Chinese Medicine, Capital Medical University, China.
    2. 2Department of Resources and Identification of Chinese Materia Medica, School of Chinese Materia Medica, Beijing University of Chinese Medicine, China.
    3. 3Department of Chemistry of Chinese Materia Medica, Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines, Beijing, PR, China.

    CORRESPONDENCE

    Muxin Gong

    Department of Pharmaceutics of TCM, Beijing Key Lab of TCM Collateral Disease Theory Research, School of Traditional Chinese Medicine, Capital Medical University, China.

    gongmuxin@ccmu.deu.cn

    Received: 28-01-2021; Revised: 19-07-2021; Accepted: 26-07-2021.

    Volume 17, Issue 75 · pp. 615–622 · PUBLISHED 11 November 2021 · DOI: 10.4103/pm.pm_47_21

    View on Pharmacogn. Mag. original site ↗

    ABSTRACT

    Objectives: In this study, we aimed to determine the interaction of paeoniflorin and liquiritin during intestinal absorption. Materials and Methods: The interaction between paeoniflorin and liquiritin (100 μM) was studied using in situ single‑pass intestinal perfusion (SPIP) model use the whole small intestine and in vitro Caco‑2 cell monolayer bidirectional transport model. Results: In situ SPIP research demonstrated that liquiritin significantly increased the Ka, Papp, absorption rate, and cumulative amount of paeoniflorin up to 7.97, 8.98, 7.07, and 10.71 folds, respectively, even higher than that of verapamil, a specific P‑gp inhibitor, and control. Furthermore, 18 β‑glycyrrhetinic acid (18 β‑GA) markedly increased the Ka, Papp, absorption rate, and cumulative amount of paeoniflorin up to 3.30, 3.27, 3.42, and 4.04 folds, respectively. Bidirectional transport studies indicated that liquiritin and paeoniflorin could prompt the absorption of each other by increasing the Papp (AP‑BL) of paeoniflorin and liquiritin from (3.83 ± 0.51) ×10−7 to (5.60 ± 0.51) ×10−7 cm/s and (3.86 ± 0.34) ×10−7 to (8.26 ± 0.51) ×10−7 cm/s, respectively. The 18 β‑GA significantly prompted the Papp (AP‑BL) of paeoniflorin to (5.54 ± 0.92) ×10−7 cm/s. Conclusion: Liquiritin and paeoniflorin increased the absorption of each other. This could provide essential reference to predict the oral bioavailability, the pharmacokinetics, and the clinical application of coadministration of liquiritin‑and paeoniflorin‑containing SGT and other herbal formulas.

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      He, R., Wang, S., Liu, Q., Xie, K., Xu, Y., Shi, J., Wang, Z., & Gong, M. (2021). Liquiritin Enhancing Intestinal Absorption of Paeoniflorin in in situ Single‑pass Intestinal Perfusion and in vitro Caco‑2 Cell Monolayer Absorption Models. Pharmacognosy Magazine, 17(75), 615–622. https://doi.org/10.4103/pm.pm_47_21