Michiels M, Hendriks R, Heykants J, van den Bossche H
Arch Int Pharmacodyn Ther. 1982 Apr;256(2):180-91.
A sensitive and specific radioimmunoassay procedure was developed for mebendazole and flubendazole enabling a more thorough study of the systemic absorption and pharmacokinetic behaviour of the drugs. In rats, plasma levels of oral and subcutaneous mebendazole were about 10 times higher than those of flubendazole. The pro-drug R 34 803 showed levels of metabolically formed flubendazole similar to those found for mebendazole. Intramuscular flubendazole in dogs, injected for 5 consecutive days, produced sustained fairly high plasma levels for at least 6 weeks 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, however, produced only an increase by 1.4 of the plasma levels and AUC-values, indicating that the absorption of flubendazole is limited by the extremely poor solubility of the drug in the contents of the gastrointestinal tract.
已开发出一种灵敏且特异的放射免疫分析方法用于检测甲苯达唑和氟苯达唑，从而能够更全面地研究这些药物的全身吸收情况和药代动力学行为。在大鼠中，口服和皮下注射甲苯达唑后的血浆水平比氟苯达唑高约10倍。前体药物R 34 803代谢形成的氟苯达唑水平与甲苯达唑相似。在犬中连续5天肌肉注射氟苯达唑，在最后一剂后至少6周内血浆水平持续保持相当高。当氟苯达唑与食物一起服用时，其在人体中的口服吸收明显增强。然而，剂量增加20倍时，血浆水平和AUC值仅增加1.4倍，这表明氟苯达唑的吸收受到该药物在胃肠道内容物中极低溶解度的限制。
