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剂型对人体中甲苯咪唑生物利用度的影响。

The effect of dose form on the bioavailability of mebendazole in man.

作者信息

Dawson M, Watson T R

出版信息

Br J Clin Pharmacol. 1985 Jan;19(1):87-90. doi: 10.1111/j.1365-2125.1985.tb02617.x.

Abstract

Four different dose forms of mebendazole were administered to human volunteers, and urine was collected and assayed for mebendazole and unconjugated metabolites of mebendazole. Oral administration of mebendazole as an oily suspension slightly enhances the bioavailability of the drug, however mebendazole is not absorbed following rectal administration. The major urinary metabolite of mebendazole in humans is 2-amino-5(6)[alpha-hydroxybenzyl]benzimidazole (IV), not 2-amino-5(6) benzoylbenzimidazole (II), as previously reported.

摘要

将四种不同剂型的甲苯咪唑给予人类志愿者,并收集尿液检测甲苯咪唑及其未结合代谢物。甲苯咪唑以油悬液形式口服可略微提高药物的生物利用度,然而,甲苯咪唑经直肠给药后不被吸收。人类尿液中甲苯咪唑的主要代谢物是2-氨基-5(6)[α-羟基苄基]苯并咪唑(IV),而非先前报道的2-氨基-5(6)苯甲酰基苯并咪唑(II)。

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