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Titolo:
PASSAGE OF S-(-KETOPROFEN AND R-(-)-KETOPROFEN ACROSS THE HUMAN ISOLATED-PERFUSED PLACENTA())
Autore:
LAGRANGE F; PEHOURCQ F; BANNWARTH B; LENG JJ; SAUX MC;
Indirizzi:
CHU PELLEGRIN,LAB PHARMACOCINET & PHARM CLIN F-33076 BORDEAUX FRANCE CHU PELLEGRIN,LAB PHARMACOCINET & PHARM CLIN F-33076 BORDEAUX FRANCE CHU PELLEGRIN,PHARMACOL LAB F-33076 BORDEAUX FRANCE CHU PELLEGRIN,LAB THERAPEUT,EA 525 F-33076 BORDEAUX FRANCE CHU PELLEGRIN,SERV GYNECOL OBSTET F-33076 BORDEAUX FRANCE UNIV VICTOR SEGALEN F-33076 BORDEAUX FRANCE
Titolo Testata:
Fundamental and clinical pharmacology
fascicolo: 3, volume: 12, anno: 1998,
pagine: 286 - 291
SICI:
0767-3981(1998)12:3<286:POSARA>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
NONSTEROIDAL ANTIINFLAMMATORY DRUGS; ANTI-INFLAMMATORY DRUGS; PROTEIN-BINDING; KETOPROFEN; PHARMACOKINETICS; ANTIPYRINE; FLUID; SERUM;
Keywords:
NONSTEROIDAL ANTIINFLAMMATORY DRUG; STEREOSELECTIVITY; PLASMA PROTEIN BINDING; KETOPROFEN; PLACENTAL TRANSFER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
F. Lagrange et al., "PASSAGE OF S-(-KETOPROFEN AND R-(-)-KETOPROFEN ACROSS THE HUMAN ISOLATED-PERFUSED PLACENTA())", Fundamental and clinical pharmacology, 12(3), 1998, pp. 286-291

Abstract

Ketoprofen is a chiral non-steroidal anti-inflammatory drug (NSAID) available as a racemic (rac) mixture of S-(+)- and R-(-)isomers. Its inhibitory effect on prostaglandin biosynthesis resides virtually in theS-form. Interestingly, R-ketoprofen does not undergo substantial metabolic inversion in humans. Though contraindicated during the last trimester of pregnancy, NSAIDs, including ketoprofen, are used as tocolytic agents in some cases. The S/R plasma concentration ratio was reported to average 2.3 in premature neonates whose mothers were given rac-ketoprofen and to be close to 1 in the maternal plasma. Thus, we investigated the placental transfer of rac-ketoprofen in vitro using Schneider's perfused human cotyledon model. Glucosed Earle solutions with and without human serum albumin (HSA) were used. Several maternal perfusates were tested with different rac-ketoprofen concentrations together with 20 mg L-1 of antipyrine as a reference substance. Ketoprofen enantiomers were assayed by a specific HPLC method with derivatization procedure. HSA concentrations in maternal perfusate influenced the placental transfer of ketoprofen enantiomers. In the absence of HSA in the maternal perfusate, the S-(+)/R-(-) concentration ratio was close to I in the fetal perfusate. By contrast this ratio averaged 1.44 after addition of BSA 10 g L-1 on the maternal side. Similar results were found for dialysis experiments using an inert Spectrapor 2 membrane suggesting that the S-(+)-free concentration is superior to the R-(-)-free concentration in the presence of HSA. Direct measurements of the free concentrations by centrifugal ultrafiltration confirmed this hypothesis. Accordingly, the data observed in vivo may result, at least in part, from the stereoselective protein binding of ketoprofen. (C) 1998 Elsevier, Paris.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 00:17:40