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

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

DOI: 10.1016/J.TVJL.2007.04.011

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

参考文章(11)
Miriam T Teruel, Antonio Eduardo Felipe, Huga Daniel Solana, Juan Manuel Sallovitz, Carlos Edmundo Lanusse, None, Placental and fetal toxicity of albendazole sulphoxide in Wistar rats. Veterinary and Human Toxicology. ,vol. 45, pp. 131- 136 ,(2003)
B.P.S. Capece, G. Castells, F. Pérez, M. Arboix, C. Cristòfol, Pharmacokinetic behaviour of albendazole sulphoxide enantiomers in male and female sheep. Veterinary Research Communications. ,vol. 24, pp. 339- 348 ,(2000) , 10.1023/A:1006496122684
L. Toribio, M.J. Nozal, J.L. Bernal, E.M. Nieto, Use of semipreparative supercritical fluid chromatography to obtain small quantities of the albendazole sulfoxide enantiomers. Journal of Chromatography A. ,vol. 1011, pp. 155- 161 ,(2003) , 10.1016/S0021-9673(03)01179-8
C. Cristofol, G. Virkel, L. Alvarez, S. Sanchez, M. Arboix, C. Lanusse, Albendazole sulphoxide enantiomeric ratios in plasma and target tissues after intravenous administration of ricobendazole to cattle. Journal of Veterinary Pharmacology and Therapeutics. ,vol. 24, pp. 117- 124 ,(2001) , 10.1046/J.1365-2885.2001.00320.X
B.P.S. Capece, M. Navarro, T. Arcalis, G. Castells, L. Toribio, F. Perez, A. Carretero, J. Ruberte, M. Arboix, C. Cristòfol, Albendazole Sulphoxide Enantiomers in Pregnant Rats Embryo Concentrations and Developmental Toxicity Veterinary Journal. ,vol. 165, pp. 266- 275 ,(2003) , 10.1016/S1090-0233(02)00158-2
S.F. SÁnchez, L.I. Alvarez, C.E. Lanusse, FASTING-INDUCED CHANGES TO THE PHARMACOKINETIC BEHAVIOUR OF ALBENDAZOLE AND ITS METABOLITES IN CALVES Journal of Veterinary Pharmacology and Therapeutics. ,vol. 20, pp. 38- 47 ,(1997) , 10.1046/J.1365-2885.1997.00810.X
V.L. Lanchote, O.M. Takayanagui, F.H. Mateus, Enantioselective renal excretion of albendazole metabolites in patients with neurocysticercosis. Chirality. ,vol. 16, pp. 520- 525 ,(2004) , 10.1002/CHIR.20071
Gracia Merino, Antonio J Molina, José L Garcı́a, Mivis M Pulido, Julio G Prieto, Ana I Álvarez, Intestinal elimination of albendazole sulfoxide: pharmacokinetic effects of inhibitors International Journal of Pharmaceutics. ,vol. 263, pp. 123- 132 ,(2003) , 10.1016/S0378-5173(03)00369-7
D. R. HENNESSY, J. W. STEEL, E. LACEY, G. K. EAGLESON, R. K. PRICHARD, The disposition of albendazole in sheep. Journal of Veterinary Pharmacology and Therapeutics. ,vol. 12, pp. 421- 429 ,(1989) , 10.1111/J.1365-2885.1989.TB00693.X
P. Delatour, E. Benoit, M. Caude, A. Tambute, Species differences in the generation of the chiral sulfoxide metabolite of albendazole in sheep and rats. Chirality. ,vol. 2, pp. 156- 160 ,(1990) , 10.1002/CHIR.530020306