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

• Published in: Journal of pharmaceutical investigation Vol. 46; no. 3; pp. 273 - 282
• Main Authors: Heo, Seo-Hee, Lee, Dong-Seok, Ham, Seong-Ho, Cho, Jung-Hee, Kwon, Young-Dal, Lee, Yong-Bok, Cho, Hea-Young
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 01-06-2016; 한국약제학회
• Subjects: Biomedical and Life Sciences; Biomedicine; Original Article; 약학; Human; Paeoniflorin; UPLC-MS/MS; Pharmacokinetics
• ISSN: 2093-5552; 2093-6214
• DOI: 10.1007/s40005-016-0242-3

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 AUC
0−∞
, CL/F, V
d
/F, C
max
, T
max
and t
1/2
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 (V
d
/F), the maximum plasma concentration (C
max
), and the time to reach C
max
(T
max
), respectively. The elimination half-life (t
1/2
) 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.