Stereoselective distribution and stereoconversion of zopiclone enantiomers in plasma and brain tissues in rats.

作者: Christine Fernandez , Patrice Alet , Catherine Davrinche , Joelle Adrien , Alain Thuillier

DOI: 10.1211/0022357021778574

关键词: PharmacokineticsChemistryBlood plasmaOral administrationPharmacologyHypnoticDistribution (pharmacology)EnantiomerBlood samplingZopiclone

摘要: Concentrations of (-)-zopiclone and (+)-zopiclone were determined in plasma brain after oral administration, to investigate the stereoselectivity distribution rats. Zopiclone enantiomers administered separately rats concentrations by chiral HPLC brain. In initial experiments, treated with urethane before cannulation for blood sampling but as this drug modified zopiclone pharmacokinetics, it was not used subsequent studies. This study showed that pharmacokinetics gavage are stereoselective. After administration (+)-zopiclone, no stereoconversion observed plasma. Conversely, (-)-zopiclone, both found (+)-zopiclone/(-)-zopiclone ratios 1 8.4 brain, respectively. Our findings suggest undergoes is stereospecifically distributed

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