Comparative Pharmacokinetics of Two Fast-Dissolving Oral Ibuprofen Formulations and a Regular-Release Ibuprofen Tablet in Healthy Volunteers
Rent the article at a discountRent now
* Final gross prices may vary according to local VAT.Get Access
Spalt-Liqua® is a new soft gelatin capsule containing 200mg of totally dissolved ibuprofen as the active ingredient. The primary objective of the study was to assess bioequivalence between the new ibuprofen formulation and the standard 200mg sugar-coated tablets. The secondary objective was to assess bioequivalence between the new formulation and 200mg tablets of a fast-dissolving ibuprofen lysinate formulation.
Design and Study Participants
A single oral dose of ibuprofen 400mg (two of each type of capsule or tablet) was administered to 26 healthy male volunteers in a nonblind, randomised, three-way crossover study with a 6-day washout interval between each drug administration period.
Main Outcome Measures and Results
For the soft gelatin capsules, maximum concentration (Cmax) was significantly greater and time to reach maximum concentration (tmax) was significantly shorter in comparison with the reference tablet formulation, and therefore bioequivalence for these parameters could not be confirmed. However, the shorter absorption time and higher peak plasma concentration did not affect the extent of absorption of the soft gelatin capsule. In contrast to this result, the pharmacokinetic profile of the soft gelatin capsules was very similar to that of the fast-dissolving ibuprofen lysinate tablets. The 90% confidence intervals for logarithmically transformed Cmax and areas under the drug concentration-time curve from zero to the time of the last measurable concentration (AUCt) and to infinity (AUC∞) were within the required bioequivalence range. The three formulations were well tolerated and no clinically significant adverse events were observed.
In accordance with previous results, this study confirmed the pharmacokinetic differences between a standard ibuprofen tablet formulation and fast-dissolving formulations.
- Busson M. Update on ibuprofen: review article. J Int Med Res 1986; 14: 53–62
- Albert KS, Gernaat CM. Pharmacokinetics of ibuprofen. Am J Med 1984; 77: 40–6 CrossRef
- Davies NM. Clinical pharmacokinetics of ibuprofen. The first 30 years. Clin Pharmacokinet 1998; 34: 101–54 CrossRef
- Geisslinger G, Dietzel K, Bezler H, et al. Therapeutically relevant differences in the pharmacokinetical and pharmaceutical behavior of ibuprofen lysinate as compared to ibuprofen acid. Int J Clin Pharmacol Ther Toxicol 1989; 27: 324–8
- Chiarini A, Tartarini A, Fini A. pH-solubility relationship and partition coefficients for some anti-inflammatory arylaliphatic acids. Archiv Pharmazie 1984; 317: 268–73 CrossRef
- Ceppi MN, Gazzaniga A, Gianesello V, et al. Activity and pharmacokinetics of a new oral dosage form of soluble ibuprofen. Arzneimittelforschung 1992; 42: 556–9
- Laska EM, Sunshine A, Marrero I, et al. The correlation between blood levels of ibuprofen and clinical analgesic response. Clin Pharmacol Ther 1986; 40: 1–7 CrossRef
- Hummel T, Cramer O, Mohammadian P, et al. Comparison of the antinociception produced by two oral formulations of ibuprofen: ibuprofen effervescent vs ibuprofen tablets. Eur J Clin Pharmacol 1997; 52: 107–14 CrossRef
- Comparative Pharmacokinetics of Two Fast-Dissolving Oral Ibuprofen Formulations and a Regular-Release Ibuprofen Tablet in Healthy Volunteers
Clinical Drug Investigation
Volume 21, Issue 1 , pp 73-78
- Cover Date
- Print ISSN
- Online ISSN
- Springer International Publishing
- Additional Links
- Industry Sectors