消旋阿苯达唑亚砜对映体及单独给药在大鼠体内的药代动力学
Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats.
作者信息
Capece Bettencourt P S, Castells Gloria, Godoy Carlo, Arboix Margarita, Cristòfol Carles
机构信息
Secção de Farmacologia e Toxicologia, Departamento de Para-Clínicas, Faculdade de Veterinária, Universidade Eduardo Mondlane, Maputo, Mozambique.
出版信息
Vet J. 2008 Aug;177(2):297-9. doi: 10.1016/j.tvjl.2007.04.011. Epub 2007 Jun 12.
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).
在大鼠口服10mg/kg消旋阿苯达唑亚砜（rac-ABZSO）、5mg/kg（-）-阿苯达唑亚砜或5mg/kg（+）-阿苯达唑亚砜后，研究了阿苯达唑亚砜（ABZSO）对映体的药代动力学行为。在所有处理中，ABZSO对映体的处置情况相似，但在所有情况下，计算得出的（-）-ABZSO的曲线下面积均高于（+）-ABZSO。结果表明，ABZSO对映体不存在手性转化。给予消旋阿苯达唑亚砜后，尿中回收的总剂量的17.2%为阿苯达唑（ABZ）（0.1%）、阿苯达唑砜（ABZSO₂）（0.3%）、阿苯达唑2-氨基砜（ABZ-SO₂NH₂）（3.1%）和ABZSO（13.7%）。尿中（+）与（-）的比例（1.6）与血液中（1.7）相似。
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