Abstract
BACKGROUND: A new oral paracetamol formulation with the same paracetamol quantity (24 mg/mL) as a marketed formulation but with finer active ingredient particle size and lower amounts of maltitol (5.85 g/dose in the test formulation vs 7.25 g/dose in the reference formulation) and sorbitol (2.4 g/dose vs 2.83 g/dose) was developed. OBJECTIVE: Establish the bioequivalence of the new pediatric formulation (test treatment) compared with the marketed formulation (reference treatment). METHODS: This Phase I, open-label trial assigned healthy adult volunteers to a single 42-mL (1 g para-cetamol) dose of test or reference treatment. Participants received both treatments in a randomized order separated by a 72-hour washout period. The primary endpoints were AUC(0-tlast) (AUC vs time curve from time 0 to last measurable sampling timepoint), C(max), and t(max). Safety assessments included adverse event, clinical laboratory, and physical examination data. RESULTS: Thirty-five participants were randomized and treated. The study population was 42.9% women (57.1% men) with a median age of 30 years; most participants were non-Hispanic White. Mean C(max) values were comparable between test and reference products, with a median t(max) of 1.00 hour for both. The test/reference ratios (%) (90% CI) for AUC(0-tlast) and C(max) were 98.69% (96.46, 100.97) and 100.73% (95.63, 106.10), respectively. There were no adverse events or deaths. CONCLUSIONS: The new paracetamol formulation is bioequivalent to the marketed formulation.