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Pharmacokinetic evaluation of paeoniflorin after oral administration of Paeoniae Radix extract powder to healthy Korean subjects using UPLC-MS/MS

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Abstract

Paeoniae Radix, a traditional herbal medicine, has been used in antispasmodic action, alleviating pain, and activating circulation. The aim of this study was to evaluate the pharmacokinetics (PKs) of paeoniflorin in healthy Korean subjects and develop an analytical method for the quantification of paeoniflorin in human plasma. This was an open-label, randomized, and single-dose study in 10 healthy Korean subjects who received a Paeoniae Radix extract powder. The plasma concentration of paeoniflorin up to 12 h was determined using a validated ultra-performance liquid chromatography tandem mass spectrometric method. The PK parameters such as AUC0−∞, CL/F, Vd/F, Cmax, Tmax and t1/2 were calculated using WinNonlin® software (version 6.4, Pharsight®, a Certara™ Company). The best PK model of paeoniflorin in humans was the one-compartment model. The mean parameters were 2625.71 L/h, 10,150.55 L, 6.97 ng/mL, and 1.64 h for the oral clearance (CL/F), the volume of distribution (Vd/F), the maximum plasma concentration (Cmax), and the time to reach Cmax(Tmax), respectively. The elimination half-life (t1/2) was 2.68 h. The validated method was successfully applied to the PK study of paeoniflorin in humans. The lower limit of quantification for paeoniflorin in human plasma was 0.2 ng/mL. This study was the first to evaluate the PKs of paeoniflorin after the usual oral dose of Paeoniae Radix extract powder (3.4 g containing 108.18 mg paeoniflorin) in Korean subjects.

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Acknowledgments

All authors (S. -H.Heo, S. -J. Kim, D. -S. Lee, Y. -D. Kwon, S. -H. Ham, J. -H. Cho, Y. -B. Lee, H. -Y. Cho) declare that they have no conflicts of interest.This work was supported by the Jeollanam-Do Development Institute for Korean Traditional Medicine (JKTM) grant funded by the Korean government (MOHW).

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Authors and Affiliations

  1. College of Pharmacy, CHA University, 335 Pangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-do, 13488, Republic of Korea

    Seo-Hee Heo, Dong-Seok Lee & Hea-Young Cho

  2. Jeonnam Development Institute for Korean Traditional Medicine, 288 Udeuraendeu-gil, Jangheung-gun, Jeollanam-do, 59338, Republic of Korea

    Seong-Ho Ham & Jung-Hee Cho

  3. Department of Oriental Rehabilitation Medicine, Wonkwang University Hospital, 1140-23 Hoejae-ro, Nam-gu, Gwangju, 61729, Republic of Korea

    Young-Dal Kwon

  4. College of Pharmacy and Institute of Bioequivalence and Bridging Study, Chonnam National University, 77 Yongbong-ro, Buk-gu, Gwangju, 61186, Republic of Korea

    Yong-Bok Lee

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  1. Seo-Hee Heo
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Heo, SH., Lee, DS., Ham, SH. et al. Pharmacokinetic evaluation of paeoniflorin after oral administration of Paeoniae Radix extract powder to healthy Korean subjects using UPLC-MS/MS. Journal of Pharmaceutical Investigation 46, 273–282 (2016). https://doi.org/10.1007/s40005-016-0242-3

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  • DOI: https://doi.org/10.1007/s40005-016-0242-3

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