Abstract
BACKGROUND: A novel ibuprofen (IBU) formulation, Advil(®) Film-Coated Tablets (IBUNa), was developed. OBJECTIVE: Pharmacokinetic comparison of IBUNa versus other IBU formulations. STUDY DESIGN: Two randomized, single-dose, open-label, five-way crossover pharmacokinetic studies. SETTING: Inpatient research clinic. SUBJECTS: Seventy-one healthy adult volunteers. INTERVENTION: Study 1: In three periods, fasted subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg, Advil(®) Liqui-Gels(®) (IBULG) 2 × 200 mg, and Motrin(®) IB (IBUMot) 2 × 200 mg tablets. In two periods following a high-fat breakfast, subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg and IBULG 2 × 200 mg. Study 2: In five study periods, fasted subjects received 400-mg IBU dose equivalents as IBUNa 2 × 256 mg, Advil(®) FastGel(®) (IBUFG) 2 × 200 mg, Nurofen(®) (IBUNur) 2 × 200 mg, Advil(®) (IBUAdv) 2 × 200 mg, and Nurofen(®) Express containing IBU lysinate (IBULys) 2 × 342 mg. MAIN OUTCOME MEASURE: Log-transformed area under the plasma concentration versus time curve to last observable concentration (AUCL) and maximum plasma concentration (C max) were the primary pharmacokinetic parameters; time to maximum measured plasma concentration (T max) was analyzed post hoc. RESULTS: IBUNa was bioequivalent to IBULG (fasted and fed) and IBUFG and IBULys (fasted) for rate (C max) and extent (AUCL) of IBU absorption. After fasting, AUCL was bioequivalent for IBUNa and IBUMot, IBUAdv, and IBUNur, but C max occurred significantly earlier with IBUNa. After fasting, median IBUNa T max was comparable to that for IBULG, IBUFG, and IBULys, but was much shorter than that for IBUMot, IBUNur, and IBUAdv. Food slowed absorption of IBUNa and IBULG similarly. All treatments were tolerated similarly. CONCLUSION: IBUNa is absorbed faster but to a similar extent as standard IBU formulations.