Premium
A single and multiple dose study to investigate the pharmacokinetics of a prolonged release formulation of ropinirole in healthy Chinese subjects
Author(s) -
Liu Hongzhong,
Jiang Ji,
Wang Hongyun,
Chen Xia,
Liu Tao,
Cao Haijun,
Palmer Jonathan,
Gu Anita,
Hu Pei
Publication year - 2013
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.28
Subject(s) - ropinirole , medicine , pharmacokinetics , tolerability , dosing , adverse effect , pharmacology , urology , anesthesia , gastroenterology , parkinson's disease , levodopa , disease
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 t max was 8 hours and meant1 2was 5.26 hours. After 7 days dosing, median t max was 6 hours ( t1 2not determined). Systemic exposure, AUC and C max , following multiple and single dosing was similar (mean AUC (0–τ) (h ng/mL): 23.84 vs. AUC (0–∞) : 22.13; C max (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; C max (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; C max (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.