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Effects of absorption rate on the pre-systemic chiral inversion of ibuprofen in rabbits

Kosuke Doki1, Toru Hayakawa, Wenhui Lin

  • 1Department of Pharmacology and Therapeutics, Hokkaido College of Pharmacy, 7-1 Katsuraoka, Otaru 047-0264, Hokkaido, Japan.

The Journal of Pharmacy and Pharmacology
|September 6, 2003
PubMed

The chiral inversion kinetics of ibuprofen was evaluated after intraduodenal administration of racemic ibuprofen in conventional powder form and sustained-released granules compared with intravenous administration in rabbits. The AUC ratios of the S-(+) and R-(-) enantiomers remained almost constant values with time up to 2 h after administration of sustained-release formulation, while those after administration of the powder increased with time. R-(-) enantiomer to S-(+) enantiomer inversion ratios after intraduodenal administration of the powder form and the sustained-release form, and after intravenous injection were calculated to be 1.63, 1.94 and 1.19, respectively, indicating that pharmacological effects may depend on the absorption rate in rabbits.

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