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Titolo:
Stereoselective disposition of tiaprofenic acid enantiomers in rats
Autore:
Erb, K; Brugger, R; Williams, K; Geisslinger, G;
Indirizzi:
Univgen,angen Nurnberg, Dept Expt & Clin Pharmacol & Toxicol, D-91054 Erlan Univ Erlangen Nurnberg Erlangen Germany D-91054 & Toxicol, D-91054 Erlan St Vincent Hosp, Dept Clin Pharmacol, Sydney, NSW, Australia St Vincent Hosp Sydney NSW Australia n Pharmacol, Sydney, NSW, Australia
Titolo Testata:
CHIRALITY
fascicolo: 2, volume: 11, anno: 1999,
pagine: 103 - 108
SICI:
0899-0042(1999)11:2<103:SDOTAE>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
METABOLIC CHIRAL INVERSION; 2-ARYLPROPIONIC ACIDS; PHARMACOLOGICAL PROPERTIES; RHEUMATIC DISEASES; COA SYNTHETASE; COENZYME-A; PHARMACOKINETICS; CONSEQUENCES; DERIVATIVES; IBUPROFEN;
Keywords:
tiaprofenic acid enantiomers; stereoselective disposition; metabolic chiral inversion;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Geisslinger, G UnivD-91054en Nurnberg, Dept Expt & Clin Pharmacol & Toxicol, Univ Str 22, Univ Erlangen Nurnberg Univ Str 22 Erlangen Germany D-91054
Citazione:
K. Erb et al., "Stereoselective disposition of tiaprofenic acid enantiomers in rats", CHIRALITY, 11(2), 1999, pp. 103-108

Abstract

The pharmacokinetics and metabolic chiral inversion of the S(+)- and R(-)-enantiomers of tiaprofenic acid (S-TIA, R-TIA) were assessed in vivo in rats, and in addition the biochemistry of inversion was investigated in vitro in rat liver homogenates. Drug enantiomer concentrations in plasma were investigated following administration of S-TIA and R-TIA (i.p. 3 and 9 mg/kg) over 24 hr. Plasma concentrations of TIA enantiomers were determined by stereospecific HPLC analysis. After administration of R-TIA it was found that 1) there was a time delay of peak S-TLA plasma concentrations, 2) S-TIA concentrations exceeded R-TIA concentrations from similar to 2 hr after dosing, 3) C-max and AUC((0-infinity)) for S-TIA were greater than for R-TIA following administration of S-TIA and 4) inversion was bidirectional but favored inversion of R-TLA to S-TLA. Bidirectional inversion was also observed when TIA enantiomers were incubated with liver homogenates up to 24 hr. However, the rate of inversion favored transformation of the R-enantiomer to theS-enantiomer. In conclusion, stereoselective pharmacokinetics of R- and S-TLA were observed in rats and bidirectional inversion in rat liver homogenates has been demonstrated for the first time. Chiral inversion of TIA may involve metabolic routes different from those associated with inversion of other 2-arylpropionic acids such as ibuprofen. (C) 1999 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/08/20 alle ore 00:54:43