This study was conducted to assess the pharmacokinetic characteristics of tilidine and its active metabolites nortilidine in healthy Chinese male and female volunteers. Nine healthy volunteers (4 male and 5 female) were included in the study. Subjects were administered a single oral dose 50 mg tilidine hydrochloride oral solution. The plasma tilidine and nortilidine concentrations were determined by gas chromatography nitrogen phosphorous detection (GC-NPD). The pharmacokinetic parameters were estimated from plasma concentration-time profiles using model independent method. The main pharmacokinetic data (mean±SD) for tilidine and nortilidine were Cmax (63.39±28.99) and (122.53±23.23) ng/mL; Tmax (0.37±0.07) and (0.64±0.30) h; t1/2 (2.83±1.35) and (5.72±1.37) h; AUC0-∞ (101.59±41.85) and (577.13±189.77) ng·h/mL, respectively. The mean pharmacokinetic parameters for male and female were as follows: for tilidine: Cmax (73.88±40.88) and (55.01±15.16) ng/mL, Tmax (0.37±0.08) and (0.36±0.08) h, t1/2 (4.05±1.07) and (1.86±0.41) h, AUC0-∞ (119.00±55.11) and (87.66±26.08) ng·h/mL; for nortilidine: Cmax (108.82±27.88) and (133.49±12.56) ng/mL, Tmax (0.94±0.13) and (0.40±0.09) h, t1/2 (4.66±1.18) and (6.57±0.84) h, AUC0-∞ (601.59±281.07) and (557.57±108.16) ng·h/mL. The t1/2 for tilidine in male was significantly higher than that in female, while Tmax for nortilidine in male was significantly higher than that in female. There was no serious adverse effects, but significant difference in the incidence of adverse effects was found between male and female. There was no sufficient pharmacokinetic reason to adjust the dose of tilidine when it was administered in Chinese patients.
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