Effects of absorption rate on the pre-systemic chiral inversion of ibuprofen in rabbits.
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.
Doki
Kosuke
K
Department of Pharmacology and Therapeutics, Hokkaido College of Pharmacy, 7-1 Katsuraoka, Otaru 047-0264, Hokkaido, Japan.
Hayakawa
Toru
T
Lin
Wenhui
W
Yanaguimoto
Hitomi
H
Ding
Guohua
G
Inotsume
Nobuo
N
D000818:Animals; D003692:Delayed-Action Preparations; D004386:Duodenum / Q000187:drug effects* / Q000502:physiology; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D007408:Intestinal Absorption / Q000187:drug effects* / Q000502:physiology; D008297:Male; D011208:Powders / Q000008:administration & dosage / Q000493:pharmacokinetics; D011817:Rabbits; D013237:Stereoisomerism
D003692:Delayed-Action Preparations; D011208:Powders; D007052:Ibuprofen