Considerable interindividual variation in the pharmacokinetics of tolperisone HCl

The aim of this study was to determine the pharmacokinetic profiles of oral tolperisone hydrochloride in healthy volunteers.

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.

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.

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.