CHIRALITY OF THE SULFOXIDE METABOLITES OF FENBENDAZOLE AND ALBENDAZOLE IN SHEEP

被引:58
作者
DELATOUR, P [1 ]
BENOIT, E [1 ]
GARNIER, F [1 ]
BESSE, S [1 ]
机构
[1] NATL SCH VET MED LYON,DEPT BIOCHEM,LYONS,FRANCE
关键词
D O I
10.1111/j.1365-2885.1990.tb00790.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Delatour, P., Benoit, E., Gamier, F. & Besse, S. Chirality of the sulphoxide metabolites of fenbendazole and albendazole in sheep. J. vet. Pharmacol. Therap. 13, 361–366. Two prochiral sulphide drugs, fenbendazole (FBZ) and albendazole (ABZ) were administered orally to sheep. Blood samples were analysed for parent drug and S‐oxidation metabolites and the chirality of the sulphoxide metabolites was determined. The plasma concentrations of the enantiomers of the sulphoxides were never a racemate. On the contrary, the ratios were greater than 1 as soon as the sulphoxide compounds could be detected in plasma. They subsequently increased linearly throughout the time course of the kinetics, reaching the level 86:14 after FBZ and 95:5 after ABZ treatment. The major enantiomer represented 74% and 86% of the total AUC of SO FBZ and SO ABZ, respectively. P. Delatour, Department of Biochemistry, National School of Veterinary Medicine of Lyon, BP 83, 69280‐Marcy I'Etoile, France. Copyright © 1990, Wiley Blackwell. All rights reserved
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页码:361 / 366
页数:6
相关论文
共 22 条
[1]   STEREOCHEMISTRY, A BASIS FOR SOPHISTICATED NONSENSE IN PHARMACOKINETICS AND CLINICAL-PHARMACOLOGY [J].
ARIENS, EJ .
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1984, 26 (06) :663-668
[2]   STEREOSELECTIVITY IN OXIDATION OF SULPHOXIDES TO SULPHONES IN PRESENCE OF ASPERGILLUS NIGER [J].
AURET, BJ ;
BOYD, DR ;
HENBEST, HB .
JOURNAL OF THE CHEMICAL SOCIETY C-ORGANIC, 1968, (18) :2374-&
[3]   A CORRELATION OF TOXICITY OF ALBENDAZOLE AND OXFENDAZOLE WITH THEIR FREE METABOLITES AND BOUND RESIDUES [J].
DELATOUR, P ;
GARNIER, F ;
BENOIT, E ;
LONGIN, C .
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS, 1984, 7 (02) :139-145
[4]  
DELATOUR P, 1989, INT SEMINAR PHARM VE
[5]  
DELATOUR P, 1990, IN PRESS CHIRALITY, V2
[6]  
GALTIER P, 1986, AM J VET RES, V47, P447
[7]   THE DISPOSITION OF ALBENDAZOLE IN SHEEP [J].
HENNESSY, DR ;
STEEL, JW ;
LACEY, E ;
EAGLESON, GK ;
PRICHARD, RK .
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS, 1989, 12 (04) :421-429
[8]   DIRECT LIQUID-CHROMATOGRAPHIC RESOLUTION OF RACEMIC DRUGS USING ALPHA-1-ACID GLYCOPROTEIN AS THE CHIRAL STATIONARY PHASE [J].
HERMANSSON, J .
JOURNAL OF CHROMATOGRAPHY, 1983, 269 (02) :71-80
[9]   DIRECT SEPARATION OF ALBENDAZOLE SULFOXIDE ENANTIOMERS BY LIQUID-CHROMATOGRAPHY ON A CHIRAL COLUMN DERIVING FROM (S)-N-(3,5-DINITROBENZOYL) TYROSINE - APPLICATION TO ENANTIOMERIC ASSAYS ON PLASMA SAMPLES [J].
LIENNE, M ;
CAUDE, M ;
ROSSET, R ;
TAMBUTE, A ;
DELATOUR, P .
CHIRALITY, 1989, 1 (02) :142-153
[10]   DIRECT RESOLUTION OF ANTHELMINTIC DRUG ENANTIOMERS ON CHIRAL-AGP PROTEIN-BONDED CHIRAL STATIONARY PHASE [J].
LIENNE, M ;
CAUDE, M ;
ROSSET, R ;
TAMBUTE, A .
JOURNAL OF CHROMATOGRAPHY, 1989, 472 (01) :265-270