Development of a Biphasic Modified-Release Ibuprofen Tablet Formulation: Single-Dose and Multiple-Dose...

Area of Science:

• Pharmacology and Pharmaceutical Sciences
• Drug Delivery Systems
• Clinical Pharmacology

Background:

• Ibuprofen, a common NSAID, has a short half-life limiting its pain relief duration.
• Frequent dosing of immediate-release ibuprofen can be inconvenient for patients.
• Modified-release formulations aim to improve patient compliance and therapeutic outcomes.

Purpose of the Study:

• To evaluate the pharmacokinetic properties of a novel biphasic ibuprofen 400 mg immediate-release/sustained-release (IR/SR) tablet.
• To compare the bioavailability of the test formulation against a standard Nurofen 200 mg immediate-release product.
• To assess the impact of food on the absorption of the test formulation.

Main Methods:

• Open-label, randomized, crossover pharmacokinetic studies involving single and multiple doses.
• Comparison of the test formulation with two Nurofen 200 mg immediate-release tablets.
• Bioavailability assessment under fed and fasted conditions for the test formulation.

Main Results:

• The biphasic ibuprofen IR/SR tablet demonstrated bioequivalence to the reference product in terms of total, peak, and minimum steady-state exposure after repeated dosing.
• Single-dose administration of the test formulation also showed bioequivalence to the reference product.
• Food intake did not significantly affect the absorption rate or extent of the test formulation.

Conclusions:

• The developed biphasic ibuprofen 400 mg IR/SR tablet is a potentially advantageous alternative for managing mild to moderate pain.
• The formulation provides extended pain relief, potentially reducing dosing frequency.
• Further clinical studies are recommended to confirm practical relevance, especially for conditions requiring sustained pain management.