Reference

Interaction of Fasciola hepatica with albendazole and its metabolites

Interaction of Fasciola hepatica with albendazole and its metabolites. Fetterer, R. H.; Rew, R. S. (Anim. Parasitol. Inst., Agric. Res. Serv., Beltsville, MD, USA). J. Vet. Pharmacol. Ther., 7(2), 113-18 (English) 1984. CODEN: JVPTD9. ISSN: 0140-7783. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 12 Adult F. hepatica recovered from sheep 12 and 24 h after a single oral dose of albendazole (I) [54965-21-8] (20 mg/kg) contained significant amts. of 2 oxidized metabolites of I a sulfoxide (SX) [54029-12-8] and a sulfone (SO) [75184-71-3], but not I. Flukes incubated in vitro with 10 mM SX or SO contained these metabolites at a level 2 to 3 times the level obsd. in flukes recovered from sheep 24 h after a curative oral dose of I. The concn. of I in flukes was 10-fold greater than either SX or SO after a 24 h in vitro incubation in 10 mM of the resp. drug. Flukes exposed to I in vitro contained 2-fold higher SX levels than SX-treated flukes due to a combination of spontaneous oxidn. in media and fluke-mediated oxidn. of I. Measurement of end-products of glucose [50-99-7] metab. following 24 h incubation in 10 mM of either I, SX or SO did not show a significant difference between treated and untreated flukes.

Simultaneous determination of albendazole and its principal metabolites in plasma by normal phase high-performance liquid chromatography

Simultaneous determination of albendazole and its principal metabolites in plasma by normal phase high-performance liquid chromatography. Alvinerie, M.; Galtier, P. (Lab. Pharmacol. Toxicol., Inst. Natl. Rech. Agron., Toulouse 31300, Fr.). J. Pharm. Biomed. Anal., 2(1), 73-9 (English) 1984. CODEN: JPBADA. ISSN: 0731-7085. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) A sensitive, specific, and reproducible HPLC procedure using normal phase is described for the simultaneous detn. of albendazole [54965-21-8], albendazole sulfoxide [54029-12-8], and albendazole sulfone [75184-71-3] in sheep plasma, with mebendazole as an internal std. Anal. of plasma requires only 100 mL of sample, which is extd. with EtOAc and injected directly onto a 5-mm normal phase column, using hexane-EtOH () as eluent, with detection at 225 nm. The std. curves in plasma were linear for both albendazole and its metabolites at concns. from 0.1-10 mg/mL. Following i.v. injection of albendazole (1.9 mg/kg), albendazole levels decreased rapidly so that 1 h after administration, the concn. of unchanged drug was below the limit of detection. Albendazole sulfoxide and sulfone peaked in plasma at 1.5 and 8 h, resp.