HPLC-MS Determination and Pharmacokinetic Study of 7, 8- Dihydroxyflavone, a Naturally-Occurring Neuroprotective Agent after a Single Oral Administration in Rats

Author(s): Jianzhong Chen, Xiaomei Fu, Yixuan Dong, Mei Liu, Jian Zhang, Zhijun Liu*.

Journal Name: Current Pharmaceutical Analysis

Volume 14 , Issue 4 , 2018

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Abstract:

Background: 7, 8-dihydroxyflavone (7, 8-DHF) has been discovered to be a TrkB receptorspecific agonist and demonstrated remarkable therapeutic efficacy in vivo. These promising findings prompted the current pharmacokinetic study, in which we first established a practical LC-MS quantitative method for 7, 8-DHF then applied it in a pilot pharmacokinetic study in rats.

Methods: A simple HPLC-MS system was employed for the determination of 7, 8-DHF in rat plasma after the plasma samples were extracted with ethyl acetate by vortex-mixing. The method was thoroughly validated regarding accuracy, precision, sensitivity, linearity, selectivity, recovery, and stability.

Results: This method exhibited linearity within the concentration range of 9.024 (LLOQ) and 1128 ng/mL. The accuracy ranged from 87.9 to 105.6% of the actual values. The intra- and inter-day precisions ranged from 1.7 to 5.1% and from 2.2 to 4.4% (RSD, %). In the pharmacokinetic study, 7, 8-DHF was detectable in rat plasma for up to 24 h, with a terminal half-life of 22.8 h.

Conclusion: Overall, the results showed that this method was fully validated and successfully applied to a pilot pharmacokinetic study, which will facilitate the determination of the pharmacokinetic profile of 7, 8-DHF in future animal studies.

Keywords: 7, 8-dihydroxyflavone, HPLC-MS, neuroprotective agent, pharmacokinetics, determination, oral.

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Article Details

VOLUME: 14
ISSUE: 4
Year: 2018
Page: [343 - 348]
Pages: 6
DOI: 10.2174/1573412913666170410132032
Price: $65

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