Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats

Bettencourt P.S. Capece; Gloria Castells; Carlo Godoy; Margarita Arboix; Carles Cristòfol

doi:https://doi.org/10.1016/j.tvjl.2007.04.011

Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats

Bettencourt P.S. Capece, Gloria Castells, Carlo Godoy, Margarita Arboix, Carles Cristòfol

Department of Pharmacology, Therapeutics and Toxicology

Research output: Contribution to journal › Article › Research › peer-review

7 Citations (Scopus)

Abstract

The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO2 (0.3%), albendazole 2-aminosulfone (ABZ-SO2NH2) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). © 2007 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	297-299
Journal	Veterinary Journal
Volume	177
DOIs	https://doi.org/10.1016/j.tvjl.2007.04.011
Publication status	Published - 1 Aug 2008

Keywords

Albendazole sulfoxide
Enantiomers
Enantioselectivity
Pharmacokinetics
Rats

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@article{e49a8f3548fa4a468dd7c012e1927654,

title = "Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats",

abstract = "The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO2 (0.3%), albendazole 2-aminosulfone (ABZ-SO2NH2) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). {\textcopyright} 2007 Elsevier Ltd. All rights reserved.",

keywords = "Albendazole sulfoxide, Enantiomers, Enantioselectivity, Pharmacokinetics, Rats",

author = "Capece, {Bettencourt P.S.} and Gloria Castells and Carlo Godoy and Margarita Arboix and Carles Crist{\`o}fol",

year = "2008",

month = aug,

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doi = "https://doi.org/10.1016/j.tvjl.2007.04.011",

language = "English",

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pages = "297--299",

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TY - JOUR

T1 - Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats

AU - Capece, Bettencourt P.S.

AU - Castells, Gloria

AU - Godoy, Carlo

AU - Arboix, Margarita

AU - Cristòfol, Carles

PY - 2008/8/1

Y1 - 2008/8/1

N2 - The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO2 (0.3%), albendazole 2-aminosulfone (ABZ-SO2NH2) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). © 2007 Elsevier Ltd. All rights reserved.

AB - The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO2 (0.3%), albendazole 2-aminosulfone (ABZ-SO2NH2) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). © 2007 Elsevier Ltd. All rights reserved.

KW - Albendazole sulfoxide

KW - Enantiomers

KW - Enantioselectivity

KW - Pharmacokinetics

KW - Rats

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DO - https://doi.org/10.1016/j.tvjl.2007.04.011

M3 - Article

VL - 177

SP - 297

EP - 299

ER -