Preliminary pharmacokinetic study of ibuprofen enantiomers after administration of a new oral formulation (ibuprofen arginine) to healthy male volunteers
✍ Scribed by Gianfranco Fornasini; Nunzia Monti; Giandomenico Brogin; Maddalena Gallina; Mario Eandi; Stefano Persiani; Massimo Bani; Carlo Della Pepa; Gianpaolo Zara; Margherita Strolin Benedetti
- Publisher
- John Wiley and Sons
- Year
- 1997
- Tongue
- English
- Weight
- 155 KB
- Volume
- 9
- Category
- Article
- ISSN
- 0899-0042
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✦ Synopsis
The pharmacokinetics of ibuprofen enantiomers were investigated in a crossover study in which seven healthy male volunteers received single oral doses of 800 mg racemic ibuprofen as a soluble granular formulation (sachet) containing L-arginine (designated trade name: Spedifen), 400 mg (-)R-ibuprofen arginine or 400 mg (+)Sibuprofen arginine.
Plasma levels of both enantiomers were monitored up to 480 minutes after drug intake using an enantioselective analytical method (HPLC with ultraviolet detection) with a quantitation limit of 0.25 mg/l. Substantial inter-subject variability in the evaluated pharmacokinetic parameters was observed in the present study. After (+)S-ibuprofen arginine, the following mean pharmacokinetic parameters ±SD were calculated for (+)S-ibuprofen: t max 28.6 ± 28.4 min; C max 36.2 ± 7.7 mg/l; AUC 86.4 ± 14.9 mg ⅐ h/l; t 1 ⁄2 105.2 ± 20.4 min. After (-)R-ibuprofen arginine, the following mean pharmacokinetic parameters were calculated for (+)Sibuprofen and (-)R-ibuprofen, respectively: t max 90.0