Pharmacokinetics and urinary metabolism of albendazole in man

Pharmacokinetics and urinary metabolism of albendazole in man

Albendazole, a new broad spectrum benzimidazole anthelmintic, has been administered in 10 male volunteers. Administration was randomized using 100 mg tablets, 200 mg tablets and a 2% suspension. Blood samples were obtained 0.5; 1; 1.5; 2; 2.5; 3; 3.5; 4; 5; 6; 8; 12; 24; 72 h after treatment. Albend...

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Bibliographic Details
Published in:Bulletin de la Societe de pathologie exotique et de ses filiales Vol. 76; no. 5; p. 698
Main Authors: Penicaut, B, Maugein, P, Maisonneuve, H, Rossignol, J F
Format: Journal Article
Language:French
Published: France 01-11-1983
Subjects:
Adult
Albendazole
Anthelmintics - metabolism
Anthelmintics - urine
Benzimidazoles - blood
Benzimidazoles - metabolism
Benzimidazoles - urine
Chemical Phenomena
Chemistry
Clinical Trials as Topic
Half-Life
Humans
Kinetics
Male
Random Allocation
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Summary:Albendazole, a new broad spectrum benzimidazole anthelmintic, has been administered in 10 male volunteers. Administration was randomized using 100 mg tablets, 200 mg tablets and a 2% suspension. Blood samples were obtained 0.5; 1; 1.5; 2; 2.5; 3; 3.5; 4; 5; 6; 8; 12; 24; 72 h after treatment. Albendazole sulfoxide, one of the mains albendazole blood metabolites, was assayed by HPLC and the blood half life was calculated as 8 1/2 h. The three different pharmaceutical formulations were considered bioequivalent. Urines were collected, and using T. L. C. Technics, main metabolites were identified and characterized. Hydrolysis of the carbamate function and oxidation of the sulfur atom, the alkyle chain and the aromatic ring were the main biotransformations observed.