Objective: The aim of this study was to determine the pharmacokinetic profiles of oral tolperisone hydrochloride in healthy volunteers.
Methods: After the oral administration of tolperisone hydrochloride, the plasma concentrations of tolperisone were measured in 15 healthy male Korean volunteers. The tolperisone concentration was determined using high-performance liquid chromatography with a C18 reverse-phase column.
Results: Very large interindividual differences in the AUC and Cmax were detected after oral tolperisone HCl. The AUC0-infinity, varied from 125.9-1,241.3 ng/ml x h, and the Cmax varied from 64.2 and 784.9 ng/ml. The tmax of tolperisone was 0.90 +/- 0.31 h and the mean half-life was 1.00 +/- 0.28 h.
Conclusion: These results suggest that the pharmacological effect of oral tolperisone HCl varies between individuals, and the oral tolperisone HCl dose might need to be individualized.