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Pharmacokinetics of R‐ (−)ondansetron compared with that of S‐ (−)ondansetron in rats using an LC–MS/MS method
Author(s) -
Duan Mingyu,
Zhao Qi,
Zhong Dafang,
Yuan Yue
Publication year - 2019
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.4426
Subject(s) - ondansetron , chemistry , pharmacokinetics , enantiomer , stereoselectivity , pharmacology , chromatography , high performance liquid chromatography , plasma concentration , stereochemistry , anesthesia , biochemistry , medicine , nausea , catalysis
The pharmacokinetics of R‐ (−)ondansetron ( R‐ ond) compared with that of S‐ (−)ondansetron ( S‐ ond) was studied in rats. R‐ ond and S‐ ond were injected intravenously into rats at a dose of 2.0 mg/kg. The stability of ondansetron enantiomers in rat was determined by chiral HPLC, and the concentrations of R‐ ond and S‐ ond in plasma were determined by an LC/MS/MS method. The pharmacokinetic parameters were calculated and analyzed statistically using the t‐ test. The enantiomer inversions between R‐ ond and S‐ ond did not occur in rat. The pharmacokinetic parameters ( t 1/2 , AUC, MRT, CL ) of R‐ ond and S‐ ond differed significantly. The concentration in plasma of the R / S‐ enantiomeric ratio reached a maximum value of 9.5 at 4.0 h post‐dose. The pharmacokinetics of R‐ ond and S‐ ond are stereoselective in rat, which indicates substantial stereoselectivity in the disposition of ondansetron enantiomers in rat. R‐ ond has more potential than S‐ ond to be developed as a single enantiomer drug.