[Comparative biological availability of two different ibuprofen granules].

Area of Science:

• Pharmacology
• Pharmacokinetics
• Drug Development

Background:

• Ibuprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID).
• Effervescent formulations offer potential advantages in drug delivery and absorption.
• Evaluating the bioavailability of new drug formulations is crucial for therapeutic efficacy.

Purpose of the Study:

• To compare the bioavailability of a novel ibuprofen lysine salt effervescent granule formulation (Imbun) against a standard ibuprofen preparation.
• To assess pharmacokinetic parameters including Cmax, tmax, and AUC of ibuprofen after administration of the test and reference products.

Main Methods:

• A randomized pharmacokinetic study involving 12 healthy volunteers.
• Administration of two sachets of Imbun (292.6 mg ibuprofen each) and one sachet of reference granules (600 mg ibuprofen).
• Serial blood sampling up to 10 hours post-dose, with ibuprofen plasma concentrations analyzed by HPLC.

Main Results:

• The test preparation (Imbun) showed a Cmax of 60 ± 17 µg/ml at 27 ± 17 min, while the reference product yielded 52 ± 12 µg/ml at 94 ± 27 min.
• Area under the curve (AUC) values were comparable: 150 ± 44 µg·h/ml for Imbun and 148 ± 33 µg·h/ml for the reference.
• Relative bioavailability of Imbun was 101.8% (104.1% corrected for dose), with no significant difference in absorption extent (AUC, Cmax).

Conclusions:

• The Imbun effervescent granules exhibit comparable ibuprofen bioavailability to the reference product.
• Significant differences in the rate of absorption (tmax) were observed, with Imbun showing faster absorption.
• The novel Imbun formulation is a viable alternative for ibuprofen delivery, demonstrating similar overall drug exposure.