A single and multiple dose study to investigate the pharmacokinetics of a prolonged release formulation of ropinirole in healthy Chinese subjects

摘要

An open-label, single, and 7-day multiple dose study was conducted to investigate the pharmacokinetics, safety and tolerability of a prolonged release formulation of ropinirole 2mg in healthy Chinese male (n=12) and female (n=12) subjects. After single doses, median tmax was 8hours and mean was 5.26hours. After 7 days dosing, median tmax was 6hours ( not determined). Systemic exposure, AUC and Cmax, following multiple and single dosing was similar (mean AUC(0-τ) (hng/mL): 23.84 vs. AUC(0-∞): 22.13; Cmax (ng/mL) 1.48 vs. 1.21, respectively). Systemic exposure was higher in females than males following single doses (mean AUC(0-24) (hng/mL): 21.45 vs. 15.48; P=0.009; Cmax (ng/mL): 1.40 vs. 0.99; P=0.014, respectively), but similar at steady state (mean AUC(0-τ) (hng/mL): 24.96 vs. 22.62; Cmax (ng/mL): 1.56 vs. 1.39, respectively). Estimated accumulation ratio was 1.29 (90% CI: 1.11, 1.51). Ropinirole did not display time-dependent pharmacokinetics (estimated steady state ratio: 1.09; 90% CI: 0.93, 1.27). The most common adverse events included dizziness and oral ulcer. In conclusion, Chinese subjects displayed predictable absorption, exposure and elimination following the prolonged release formulation of ropinirole 2mg. The safety findings are consistent with the previously established safety profile for ropinirole.