Development of a Biphasic Modified‐Release Ibuprofen Tablet Formulation: Single‐Dose and Multiple‐Dose Pharmacokinetics and Food‐Effect Studies

ABSTRACT Ibuprofen is the most commonly used NSAID; however, its short biological half‐life, reflected in the short duration of pain relief, limits the comfortableness of its usage. This study evaluated the pharmacokinetic properties of a newly developed biphasic ibuprofen 400 mg immediate‐release/sustained‐release (IR/SR) modified‐release tablets (test formulation), which was developed with an aim to overcome a need for frequent dosing. Both single‐dose and multiple‐dose, open‐label, randomized, crossover studies compared the bioavailability of the test formulation with two Nurofen 200 mg, immediate‐release coated tablets (reference formulation) administered within 4 h intervals. In addition, the effect of food on the test formulation performance was evaluated in a single‐dose, open‐label, randomized, crossover, bioavailability study. Based on the 95% confidence intervals of the geometric mean ratios, the new test formulation exhibited equivalent (80.00–125.00%) total (AUC t,ss ), peak (C max,ss ), and minimum (C min,ss ) steady‐state exposure compared to the reference product after repeated dosing. After a single dose of the test formulation, total (AUC t and AUC ∞ ) and peak (C max0‐4 ) exposure were bioequivalent to the reference. Food intake did not significantly alter the rate or extent of drug absorption from this product. The study medication was well‐tolerated. This ibuprofen test formulation may represent a potentially advantageous therapeutic alternative, providing extended relief of mild to moderate pain. While these considerations are supported by pharmacokinetic data, further clinical evaluation may help to better characterize their relevance in practice. The formulation may be particularly suitable for conditions where less frequent dosing is desirable, such as dental and back pain, or nighttime pain.