Abstract
Plasma concentrations of the enantiomers of flurbiprofen were measured following oral administration of (S)-flurbiprofen 50 mg and (R)-flurbiprofen 50 mg and 100 mg to sixteen healthy subjects. Chiral inversion did not occur to a measurable extent. Significantly higher values of AUC (55.2 +/- 17.0 vs 44.6 +/- 11.2 micrograms ml-1h) elimination half-life (5.6 +/- 1.4 vs 4.0 +/- 1.0 h) and mean residence time (7.5 +/- 1.6 vs 5.7 +/- 1.2 h) were observed after 50 mg (S)-flurbiprofen as compared with 50 mg (R)-flurbiprofen. With the exception of Cmax and AUC values pharmacokinetic data for the 50 mg and the 100 mg dose of (R)-flurbiprofen did not differ significantly. The data are of clinical relevance if (R)-flurbiprofen also has analgesic activity in humans and is to be developed as an analgesic.
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- Brune K., Beck W. S., Geisslinger G., Menzel-Soglowek S., Peskar B. M., Peskar B. A. Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition. Experientia. 1991 Mar 15;47(3):257–261. doi: 10.1007/BF01958153. [DOI] [PubMed] [Google Scholar]
- Geisslinger G., Menzel-Soglowek S., Schuster O., Brune K. Stereoselective high-performance liquid chromatographic determination of flurbiprofen in human plasma. J Chromatogr. 1992 Jan 3;573(1):163–167. doi: 10.1016/0378-4347(92)80492-9. [DOI] [PubMed] [Google Scholar]
- Jamali F., Berry B. W., Tehrani M. R., Russell A. S. Stereoselective pharmacokinetics of flurbiprofen in humans and rats. J Pharm Sci. 1988 Aug;77(8):666–669. doi: 10.1002/jps.2600770805. [DOI] [PubMed] [Google Scholar]
- Knadler M. P., Brater D. C., Hall S. D. Stereoselective disposition of flurbiprofen in normal volunteers. Br J Clin Pharmacol. 1992 Apr;33(4):369–375. doi: 10.1111/j.1365-2125.1992.tb04054.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Knadler M. P., Brater D. C., Hall S. D. Stereoselective disposition of flurbiprofen in uraemic patients. Br J Clin Pharmacol. 1992 Apr;33(4):377–383. doi: 10.1111/j.1365-2125.1992.tb04055.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Knadler M. P., Hall S. D. Stereoselective arylpropionyl-CoA thioester formation in vitro. Chirality. 1990;2(2):67–73. doi: 10.1002/chir.530020202. [DOI] [PubMed] [Google Scholar]
- Knihinicki R. D., Day R. O., Graham G. G., Williams K. M. Stereoselective disposition of ibuprofen and flurbiprofen in rats. Chirality. 1990;2(3):134–140. doi: 10.1002/chir.530020303. [DOI] [PubMed] [Google Scholar]
- Knihinicki R. D., Williams K. M., Day R. O. Chiral inversion of 2-arylpropionic acid non-steroidal anti-inflammatory drugs--1. In vitro studies of ibuprofen and flurbiprofen. Biochem Pharmacol. 1989 Dec 15;38(24):4389–4395. doi: 10.1016/0006-2952(89)90647-3. [DOI] [PubMed] [Google Scholar]
- Menzel-Soglowek S., Geisslinger G., Beck W. S., Brune K. Variability of inversion of (R)-flurbiprofen in different species. J Pharm Sci. 1992 Sep;81(9):888–891. doi: 10.1002/jps.2600810909. [DOI] [PubMed] [Google Scholar]
- Young M. A., Aarons L., Toon S. The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis. Br J Clin Pharmacol. 1991 Jan;31(1):102–104. doi: 10.1111/j.1365-2125.1991.tb03865.x. [DOI] [PMC free article] [PubMed] [Google Scholar]