Article: The effect of food or sucralfate on the bioavailability of S(+) and R(-) enantiomers of ibuprofen.
Journal of clinical pharmacology
1992 Volume 32, Issue 12, Page(s) 1110–1114
Abstract: ... concentration (tmax) for total, S(+), and R(-) enantiomer serum ibuprofen levels, drawn up to 10 hours after ... dosing. The AUC for R(-) ibuprofen was significantly lower than S(+) ibuprofen in all three treatment ... groups. The treatments had no different effects on AUC for S(+), R(+), or total ibuprofen. There was no ...
| Abstract | This randomized, multiple cross-over pharmacokinetic study was undertaken to determine if food or sucralfate alter the bioavailability of the active S(+) enantiomer of ibuprofen. Eleven healthy adult male volunteers were given three single 600-mg doses of ibuprofen (separated by 1 week) administered either in a fasting state, after a standardized breakfast, or with sucralfate 1 g. The main outcome measures were area under the concentration (AUC), maximum peak plasma concentration (Cmax), and time to reach peak concentration (tmax) for total, S(+), and R(-) enantiomer serum ibuprofen levels, drawn up to 10 hours after dosing. The AUC for R(-) ibuprofen was significantly lower than S(+) ibuprofen in all three treatment groups. The treatments had no different effects on AUC for S(+), R(+), or total ibuprofen. There was no difference in the ratio of S(+):R(-) enantiomers across different treatment groups, but the intersubject variability was significant (P < .05). The S(+) ibuprofen Cmax was greater than the R(-) ibuprofen Cmax for all treatment groups (P < .05). Sucralfate reduced the peak concentration of both S(+) and R(-) enantiomers when compared with fasting (P < .05). There was a slight but nonsignificant increase in the mean time to achieve peak concentration of both S(+) and R(-) enantiomers. Neither food nor sucralfate has a significant effect on ibuprofen enantiomer pharmacokinetics, but interindividual variability contributes significantly to the variability of enantiomer bioavailability. |
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| MeSH term(s) | Adult ; Biological Availability ; Fasting ; Food ; Humans ; Ibuprofen/administration & dosage ; Ibuprofen/pharmacokinetics ; Male ; Stereoisomerism ; Sucralfate/pharmacology |
| Chemical Substances | Sucralfate (54182-58-0) ; Ibuprofen (WK2XYI10QM) |
| Language | English |
| Publishing date | 1992-12 |
| Publishing country | England |
| Document type | Clinical Trial ; Comparative Study ; Journal Article ; Randomized Controlled Trial |
| ZDB-ID | 188980-1 |
| ISSN | 1552-4604 ; 0091-2700 ; 0021-9754 |
| ISSN (online) | 1552-4604 |
| ISSN | 0091-2700 ; 0021-9754 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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