A single and multiple dose study to investigate the pharmacokinetics of a prolonged release formulation of ropinirole in healthy Chinese subjects. Issue 2 (30th October 2013)

• Record Type: Journal Article
• Authors: Liu, Hongzhong; Jiang, Ji; Wang, Hongyun; Chen, Xia; Liu, Tao; Cao, Haijun; Palmer, Jonathan; Gu, Anita; Hu, Pei
• Is Part Of: Clinical pharmacology in drug development. Volume 3:Issue 2(2014:Mar./Apr.)
• Page Start: 84
• Page End: 92
• Publication Date: 2013-10-30
• Subjects: Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.28
• Languages: English
• ISSNs: 2160-7648

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <sec id="cpdd28-sec-0001" sec-type="section"> <p>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<sub>max</sub> was 8 hours and mean <inline-graphic xlink:href="ark:/27927/pgg4ssckxb7" mimetype="image" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /> was 5.26 hours. After 7 days dosing, median t<sub>max</sub> was 6 hours ( <inline-graphic xlink:href="ark:/27927/pgg4ssckx84" mimetype="image" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /> not determined). Systemic exposure, AUC and C<sub>max</sub>, following multiple and single dosing was similar (mean AUC<sub>(0–τ)</sub> (h ng/mL): 23.84 vs. AUC<sub>(0–∞)</sub>: 22.13; C<sub>max</sub> (ng/mL) 1.48 vs. 1.21, respectively). Systemic exposure was higher in females than males following single doses (mean AUC<sub>(0–24)</sub> (h ng/mL): 21.45 vs. 15.48; <italic>P</italic> = 0.009; C<sub>max</sub> (ng/mL): 1.40 vs. 0.99; <italic>P</italic> = 0.014, respectively), but similar at steady state (mean AUC<sub>(0–τ)</sub> (h ng/mL): 24.96 vs. 22.62; C<sub>max</sub> (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.</p> </sec> </abstract>