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  • Title: [Enantioselective pharmacokinetics of benproperine in healthy volunteers].
    Author: Du ZM, Zhong DF, Kang Y, Chen XY.
    Journal: Yao Xue Xue Bao; 2000 Dec; 35(12):909-12. PubMed ID: 12567913.
    Abstract:
    AIM: To investigate the enantioselective pharmacokinetic process of benproperine in healthy volunteers. METHODS: An enantiospecific HPLC method was developed and used to determine the plasma concentrations of each enantiomer. Six healthy Chinese male volunteers received an oral dose of 60 mg (+/-)-benproperine. The ratios of the enantiomers in plasma samples were measured on a chiral AGP column. The plasma concentration of each enantiomer was then calculated using the ratios of enantiomers and total concentration of the two enantiomers previously measured. RESULTS: The plasma levels of (-)-(S)-benproperine were always significantly higher than those of its antipode in six volunteers. The mean AUC0-t and Cmax values for (-)-(S)-benproperine were 2.18 and 2.12 times higher than those of (+)-(R)-benproperine. There was no significant difference between the T1/2 for both enantiomers, tested by paired t test (P > 0.05). Half an hour after administration of benproperine, the S/R ratio in plasma samples was as high as 3.8, and in 2 hours it drastically decreased to about 2.2, then kept on till 24 hours. CONCLUSION: Benproperine showed significant enantioselective pharmacokinetics in the human after an oral dose of the racemate.
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