Determination of tolperisone enantiomers in plasma and their disposition in rats.
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.
Yokoyama
T
T
Department of Hospital Pharmacy, Kyoto Pharmaceutical University, Japan.
Fukuda
K
K
Mori
S
S
Ogawa
M
M
Nagasawa
K
K
D000818:Animals; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D014049:Tolperisone / Q000097:blood* / Q000493:pharmacokinetics
D014049:Tolperisone