Related Experiment Video
Updated: Sep 27, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
Published on: December 3, 2020
[Enantioselective pharmacokinetics of benproperine in healthy volunteers]
1Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110015, China.
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.
Related Concept Videos
Bioavailability Study Design: Healthy Subjects Versus Patients
Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance
A study on guinea pigs examined the...
Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment
Pharmacokinetics in Pediatric Patients: Drug Metabolism
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Metabolism
Bioequivalence of Drugs: Drugs with Multiple Indications