Acta Pharm. 66 (2016) 279-287
Original research paper
Pharmacokinetic comparisons of S-oxiracetam and R-oxiracetam in beagle dogs
WUSAN WANG, HUI JI, TINGTING LI,
YUANWEI JIA and HAITANG XIE
cpujihui@sina.com; dreamerltt@163.com
1 Department of Pharmacology, College of Pharmacy,
China Pharmaceutical University, Nanjing 210000, China
2 Yijishan Hospital, Wannan Medical College,Wuhu
241002, Anhui Province, China
Accepted October 27, 2015
Published online March 24, 2016
A pharmacokinetic
comparison and conformational stability study of S-oxiracetam (S-ORT) and R-oxiracetam (R-ORT)
in beagle dogs was used to investigate the possible mechanism of different
effects of two oxiracetam enantiomers through a random
crossover design. After drug administration to beagle dogs, blood samples were
collected at different time points for pharmacokinetic analysis using the UPLC-ESI-MS/MS
method. Parts of plasma samples were used for conformation transformation
studies using a normal phase high performance liquid chromatographic (NP HPLC)
method. The study showed that oxiracetam enantiomers
maintained their original conformation when administered orally to beagle dogs.
Concentrations of S-ORT were
significantly higher than R-ORT 1.5 and
2 h after administration; the AUC0-∞
of S-ORT after oral administration
tended to be higher than that of R-ORT,
which showed that the different effects between S-ORT and R-ORT may be
partly associated with their distinctive absorption at least.
Keywords: S-oxiracetam, R-oxiracetam,
conformation, pharmacokinetics, beagle dogs