THE PHARMACOKINETICS OF MEBENDAZOLE AND FLUBENDAZOLE IN ANIMALS AND MAN

  • 1 January 1982
    • journal article
    • research article
    • Vol. 256  (2) , 180-191
Abstract
A sensitive and specific radioimmunoassay procedure was developed for mebendazole and flubendazole [broad-spectrum antihelmintics] enabling a more thorough study of the systemic absorption and pharmacokinetic behavior of the drugs. In rats, plasma levels of oral and s.c. mebendazole were .apprx. 10 times higher than those of flubendazole. The pro-drug R 34 803 [[5-[2-(4-fluorophenyl)-1,3-dioxolan-2-yl]-1H-benzimidazole-2yl]carbamate] showed levels of metabolically formed flubendazole similar to those found for mebendazole. Flubendazole in dogs, injected i.m. for 5 consecutive days, produced sustained fairly high plasma levels for at least 6 wk after the last dose. The absorption of oral flubendazole in man was markedly enhanced when the drug was taken together with a meal. A 20-times higher dose produced only an increase by 1.4 of the plasma levels and AUC[area under the curve]-values, indicating that the absorption of flubendazole is limited by the extremely poor solubility of the drug in the contents of the gastrointestinal tract.

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