A sensitive analytical method for the determination of SG-SP1 in rat plasma by HPLC-MS/MS and its application to a pharmacokinetic study
- Authors
- Kang, J.; Won, J.; Fei, X.; Noh, K.; Kim, S.-H.; Seo, S.-Y.; Kang, W.
- Issue Date
- 5-Aug-2021
- Publisher
- Elsevier B.V.
- Keywords
- HPLC-MS/MS; Pharmacokinetics; Rats; SG-SP1
- Citation
- Journal of Pharmaceutical and Biomedical Analysis, v.202
- Journal Title
- Journal of Pharmaceutical and Biomedical Analysis
- Volume
- 202
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/50894
- DOI
- 10.1016/j.jpba.2021.114151
- ISSN
- 0731-7085
1873-264X
- Abstract
- SG-SP1, a newly synthesised gallic acid derivative, blocks histamine release by reducing calcium influx in mast cells and inhibits inflammatory cytokine expression. This derivative has promising anti-allergic potential. Our research was designed to establish a quantitative determination method for SG-SP1 in rat plasma using high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS), to validate the analytical method including stability and to characterise its pharmacokinetic behaviour in rats. After simple protein precipitation with acetonitrile including an internal standard, SG-SP1 was eluted on a reversed-phase column using a mobile phase of water and acetonitrile (2:8 v/v, including 0.1 % formic acid). The protonated precursor ion [M+H]+ and major fragment ion were confirmed at m/z 588.2 and 180.1, respectively. The substance was stable under bench and storage conditions. The analytical method met the criteria of FDA-validated bioanalytical methods and was successfully applied to a pharmacokinetic study for the first time. SG-SP1 decayed in a biphasic pattern with terminal half-life of 5.1 h and clearance of about 3.2 L/h/kg. Double peaks were observed following oral administration, and the absolute oral bioavailability was ∼1 %. © 2021
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