title: Determination of tolperisone enantiomers in plasma and their disposition in rats.
abstract: A stereoselective assay for the determination of tolperisone enantiomers in plasma by high performance liquid chromatography was developed. Calibration curves obtained for the enantiomers were linear over plasma concentrations of 0.1-3.0 micrograms/ml with a detection limit of 20 ng/ml. Following intravenous bolus administration of 10 mg/kg of racemic tolperisone to rats, stereoselective disposition of tolperisone enantiomers was observed, and plasma concentrations were significantly higher for l-tolperisone than for d-tolperisone at 5, 15 and 30 min after administration. When either enantiomer was administered alone to rats, both enantiomers were found in plasma, indicating that a mutual chiral inversion occurs in the body.
authors.affiliation: Department of Hospital Pharmacy, Kyoto Pharmaceutical University, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Yokoyama
authors.forename: K
authors.initials: K
authors.lastname: Fukuda
authors.forename: S
authors.initials: S
authors.lastname: Mori
authors.forename: M
authors.initials: M
authors.lastname: Ogawa
authors.forename: K
authors.initials: K
authors.lastname: Nagasawa
mesh_terms: D000818:Animals; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D014049:Tolperisone / Q000097:blood* / Q000493:pharmacokinetics
chemical_list: D014049:Tolperisone