STEREOSELECTIVE DISPOSITION OF FLURBIPROFEN IN HEALTHY-SUBJECTS FOLLOWING ADMINISTRATION OF THE SINGLE ENANTIOMERS

被引:50
作者
GEISSLINGER, G
LOTSCH, J
MENZEL, S
KOBAL, G
BRUNE, K
机构
[1] Department of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nurnberg
关键词
FLURBIPROFEN; ENANTIOMERS; STEREOSELECTIVE; PHARMACOKINETICS;
D O I
10.1111/j.1365-2125.1994.tb04295.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Plasma concentrations of the enantiomers of flurbiprofen were measured following oral administration of (S)-flurbiprofen 50 mg and (R)-flurbiprofen 50 mg and 100 mg to sixteen healthy subjects. Chiral inversion did not occur to a measurable exent. Significantly higher values of AUC (55.2 +/- 17.0 vs 44.6 +/- 11.2 mug ml-1 h) elimination half-life (5.6 +/- 1.4 vs 4.0 +/- 1.0 h) and mean residence time (7.5 +/- 1.6 vs 5.7 +/- 1.2 h) were observed after 50 mg (S)-flurbiprofen as compared with 50 mg (R)-flurbiprofen. With the exception Of C(max) and AUC values pharmacokinetic data for the 50 mg and the 100 mg dose of (R)-flurbiprofen did not differ significantly. The data are of clinical relevance if (R)-flurbiprofen also has analgesic activity in humans and is to be developed as an analgesic.
引用
收藏
页码:392 / 394
页数:3
相关论文
共 11 条
[1]  
BRUNE K, 1991, EXPERIENTIA, V47, P258
[2]   STEREOSELECTIVE HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF FLURBIPROFEN IN HUMAN PLASMA [J].
GEISSLINGER, G ;
MENZELSOGLOWEK, S ;
SCHUSTER, O ;
BRUNE, K .
JOURNAL OF CHROMATOGRAPHY-BIOMEDICAL APPLICATIONS, 1992, 573 (01) :163-167
[3]  
HEINZEL G, 1993, TOPFIT 20 PHARMACOKI
[4]   STEREOSELECTIVE PHARMACOKINETICS OF FLURBIPROFEN IN HUMANS AND RATS [J].
JAMALI, F ;
BERRY, BW ;
TEHRANI, MR ;
RUSSELL, AS .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1988, 77 (08) :666-669
[5]   STEREOSELECTIVE ARYLPROPIONYL-COA THIOESTER FORMATION INVITRO [J].
KNADLER, MP ;
HALL, SD .
CHIRALITY, 1990, 2 (02) :67-73
[6]   STEREOSELECTIVE DISPOSITION OF FLURBIPROFEN IN UREMIC PATIENTS [J].
KNADLER, MP ;
BRATER, DC ;
HALL, SD .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1992, 33 (04) :377-383
[7]   STEREOSELECTIVE DISPOSITION OF FLURBIPROFEN IN NORMAL VOLUNTEERS [J].
KNADLER, MP ;
BRATER, DC ;
HALL, SD .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1992, 33 (04) :369-375
[8]   CHIRAL INVERSION OF 2-ARYLPROPIONIC ACID NON-STEROIDAL ANTI-INFLAMMATORY DRUGS .1. INVITRO STUDIES OF IBUPROFEN AND FLURBIPROFEN [J].
KNIHINICKI, RD ;
WILLIAMS, KM ;
DAY, RO .
BIOCHEMICAL PHARMACOLOGY, 1989, 38 (24) :4389-4395
[9]   STEREOSELECTIVE DISPOSITION OF IBUPROFEN AND FLURBIPROFEN IN RATS [J].
KNIHINICKI, RD ;
DAY, RO ;
GRAHAM, GG ;
WILLIAMS, KM .
CHIRALITY, 1990, 2 (03) :134-140
[10]   VARIABILITY OF INVERSION OF (R)-FLURBIPROFEN IN DIFFERENT SPECIES [J].
MENZELSOGLOWEK, S ;
GEISSLINGER, G ;
BECK, WS ;
BRUNE, K .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1992, 81 (09) :888-891