Pharmacokinetics of 8-O-acetylharpagide in mouse blood by UPLC–MS/MS

• Autorzy: Chen Shanjiang , Huang Miaoling , Yu Zheng , He Jiamin , Huang Binge , Wang Xianqin , Ma Jianshe , Wen Congcong

Identyfikatory

DOI

10.1556/1326.2018.00429

• Języki publikacji: EN

Abstrakty

EN

8-O-Acetylharpagide is the main active component of the herb Ajuga decumbens, which possesses anti-tumor, anti-virus, and anti-inflammation properties. In this study, ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) was used to measure the concentration of 8-O-acetylharpagide in mouse blood, with subsequent investigation of the pharmacokinetics of the drug after intravenous or oral administration. Shanzhiside methyl ester was used as an internal standard, and the acetonitrile precipitation method was used to process the blood samples. Chromatographic separation was achieved using an ultra-performance liquid chromatography ethylene-bridged hybrid (UPLC BEH) column (2.1 mm × 50 mm, 1.7 μm) with a gradient methanol–water mobile phase (containing 0.1% formic acid). The flow rate was 0.4 mL/min, and the elution time was 5.0 min. 8-O-Acetylharpagide was quantitatively measured using electrospray ionization (ESI) tandem mass spectrometry in multiple reaction monitoring (MRM) mode with positive ionization. The result indicated that, within the range of 5–500 ng/mL, the linearity of 8-O-acetylharpagide in mouse blood was satisfactory (r > 0.995), and the lower limit of quantification (LLOQ) was 5 ng/mL. Intra-day precision relative standard deviation (RSD) of 8-O-acetylharpagide in blood was lower than 9%, and the inter-day precision RSD was lower than 13%. The accuracy range was between 94.3% and 107.1%, average recovery was higher than 91.3%, and the matrix effect was between 100.8% and 110.8%. This analytical method was sensitive and fast with good selectivity and was successfully applied to perform pharmacokinetic studies of 8-O-acetylharpagide in mice. The bioavailability of 8-O-acetylharpagide was 10.8%, and the analysis of the primary pharmacokinetic parameters after oral and intravenous administration indicated that 8-O-acetylharpagide had a significant first pass effect after oral administration.

Słowa kluczowe

EN

8-O-acetylharpagide; pharmacokinetics; bioavailability; mouse; UPLC–MS/MS

• Wydawca: University of Silesia in Katowice ; Akademiai Kiado
• Czasopismo: Acta Chromatographica
• Rocznik: 2019
• Tom: Vol. 31, no. 3
• Strony: 183--188
• Opis fizyczny: Bibliogr. 25 poz., rys., tab.

Twórcy

autor

Chen Shanjiang

• Department of Cardiology, Wenzhou Central Hospital, Wenzhou 325000, China

autor

Huang Miaoling

• Analytical and Testing Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China

autor

Yu Zheng

• Laboratory Animal Centre, Wenzhou Medical University, Wenzhou 325035, China

autor

He Jiamin

• Analytical and Testing Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China

autor

Huang Binge

• Laboratory Animal Centre, Wenzhou Medical University, Wenzhou 325035, China

autor

Wang Xianqin

• Analytical and Testing Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China

autor

Ma Jianshe

• Analytical and Testing Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China

autor

Wen Congcong

• Laboratory Animal Centre, Wenzhou Medical University, Wenzhou 325035, China

Bibliografia

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Uwagi

PL

Opracowanie rekordu w ramach umowy 509/P-DUN/2018 ze środków MNiSW przeznaczonych na działalność upowszechniającą naukę (2019).