Abstract

Background: The aim was to determine the effect of feeding on chiral inversion of Ibuprofen isomers.Method: Six healthy volunteers participated in a two-treatment crossover study where a single dose of Ibuprofen racemate was given. One stage consisted in an 8-hour interval of fasting, while in the other, the drug was administered with a solution of saccharose and a standard food intake regimen was implemented. Results: Higher (p<0.01) S/R area under concentration-time curve ratios were achieved in the Fed stage (1.44) compared to the Fasting stage (0.976). Half-life of R-ibuprofen was significantly diminished (p<0.001) under fed conditions. Conclusions: Clearance of R-ibuprofen increased following the ingestion of saccharose and food, however, the increased bioavailability of S-ibuprofen due to R-to-S chiral inversion overrode its increased clearance. This increased inversion might be explained by the supplementary amount of drug molecules that reaches the enter ocytes through pancreatic/intestinal juice secretion following the ingestion of food.

How to Cite
FAGIOLINO, MARIANELA LORIER, MARTA VÁZQUEZ, MANUEL IBARRA, NATALIA GUEVARA, Pietro. Chiral Inversion of Ibuprofen after an Oral Administration under Complete Fasting and Fed Conditions in Caucasian Healthy Subjects. Global Journal of Science Frontier Research, [S.l.], sep. 2021. ISSN 2249-4626. Available at: <https://journalofscience.org/index.php/GJSFR/article/view/2994>. Date accessed: 04 dec. 2021. doi: https://doi.org/10.34257/GJSFRBVOL21IS2PG1.