Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Determination of Tolperisone Enantiomers in Plasma and Their Disposition in Rats
Teruyoshi YOKOYAMAKen-ichi FUKUDASachiyo MORIMana OGAWAKazuki NAGASAWA
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1992 Volume 40 Issue 1 Pages 272-274

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Abstract
A stereoselective assay for the detemination of tolperisone enantiomers in plasma by high performance liquid chromatography was developed. Calibration curves obtained for the enantiomers were linear over plasma concentrations of 0.1-3.0μg/ml with a detection limit of 20μg/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 30min after administration. When either enantiomer was administered alone to rats, both enantiomers were found in plasma, indicating that a mutual chiral inversiton occurs in the body.
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© The Pharmaceutical Society of Japan
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