Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats |
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| Authors: | Capece Bettencourt P S Castells Gloria Godoy Carlo Arboix Margarita Cristòfol Carles |
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| Affiliation: | aSecção de Farmacologia e Toxicologia, Departamento de Para-Clínicas, Faculdade de Veterinária, Universidade Eduardo Mondlane, Av. de Moçambique, Km 1,5, Maputo, Moçambique;bServei d’Anàlisi de Fàrmacs, Departament de Farmacologia, de Terapéutica i de Toxicologia, Facultat de Veterinária, Universitat Autònoma de Barcelona, 08193 Bellaterra, Barcelona, Spain |
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| 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 ABZSO(2) (0.3%), albendazole 2-aminosulfone (ABZ-SO(2)NH(2)) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). |
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| Keywords: | Albendazole sulfoxide Enantiomers Rats Pharmacokinetics Enantioselectivity |
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