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Titolo:
Simultaneous fitting of R- and S-ibuprofen plasma concentrations after oral administration of the racemate
Autore:
Lotsch, J; Muth-Selbach, U; Tegeder, I; Brune, K; Geisslinger, G;
Indirizzi:
Univ Frankfurt, Dept Clin Pharmacol, Ctr Pharmacol, D-60590 Frankfurt, Germany Univ Frankfurt Frankfurt Germany D-60590 col, D-60590 Frankfurt, Germany Univ Erlangen Nurnberg, Dept Expt & Clin Pharmacol & Toxicol, D-91054 Erlangen, Germany Univ Erlangen Nurnberg Erlangen Germany D-91054 -91054 Erlangen, Germany
Titolo Testata:
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
fascicolo: 4, volume: 52, anno: 2001,
pagine: 387 - 398
SICI:
0306-5251(200110)52:4<387:SFORAS>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHIRAL INVERSION; PHARMACOLOGICAL DIFFERENCES; PHARMACODYNAMIC MODEL; METABOLIC INVERSION; COENZYME-A; PHARMACOKINETICS; ENANTIOMERS; BIOAVAILABILITY; HUMANS; R(-)-IBUPROFEN;
Keywords:
bioequivalence; ibuprofen; pharmacokinetics;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
43
Recensione:
Indirizzi per estratti:
Indirizzo: Lotsch, J Univ Frankfurt Hosp, Dept Clin Pharmacol, Pharmazentrum Frankfurt, TheodorStern Kai 7, D-60590 Frankfurt, Germany Univ Frankfurt Hosp Theodor Stern Kai 7 Frankfurt Germany D-60590
Citazione:
J. Lotsch et al., "Simultaneous fitting of R- and S-ibuprofen plasma concentrations after oral administration of the racemate", BR J CL PH, 52(4), 2001, pp. 387-398

Abstract

Aims To assess the pharmacokinetic equivalence of two different formulations of ibuprofen lysinate with special focus on the expected effects. Methods Sixteen healthy volunteers received cross-over ibuprofen lysinate as either one tablet of 400 mg ('test') or two tablets of 200 mg ('reference'). Ibuprofen plasma concentrations were followed up for 10 h. Bioequivalence was assessed by standard noncompartmental methods. Ibuprofen plasma concentrations were fitted with a model that took bioinversion of R- to S-ibuprofen into account. Results Peak plasma concentrations of R- and S-ibuprofen were 18.1 and 20 mug ml(-1) (test), and 18.2 and 20 mug ml(-1) (reference). Areas under the plasma concentration vs time curves were 39.7 and 67.5 mug ml(-1) h (test),and 41.1 and 68.2 mug ml(-1) h (reference). Clearance of R-ibuprofen was 5.2 (test) and 5 l h(-1) (reference). A specific plasma concentration was reached with the test formulation about 5 min later than with the reference. Parameters from compartmental modelling were (given for R-and then for S-ibuprofen): body clearance: 4.9 and 4.64 l h(-1), central volume of distribution: 2.8 and 4.1 l, intercompartment clearance: 5.1 and 5.45 l h(-1), peripheral volume of distribution: 4.1 and 5.2 l. The absorption rate constant was 1.52 h(-1), and the test but not the reference formulation had a lag time of 0.1 h. Simulations showed similarity between formulations of the expected effects except for a calculated delay of 6 min with the test formulation. Conclusions Ibuprofen formulations were bioequivalent. The pharmacokineticmodel may serve as a basis for future pharmacokinetic/pharmacodynamic calculations after administration of racemic ibuprofen.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 13/07/20 alle ore 07:32:50