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

Abstract

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 2 mg in healthy Chinese male (n = 12) and female (n = 12) subjects. After single doses, median tmax was 8 hours and mean t12 was 5.26 hours. After 7 days dosing, median tmax was 6 hours (t12 not determined). Systemic exposure, AUC and Cmax , following multiple and single dosing was similar (mean AUC(0-τ) (h ng/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) (h ng/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) (h ng/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 2 mg. The safety findings are consistent with the previously established safety profile for ropinirole.