Wood S G, John B A, Chasseaud L F, Brodie R R, Baker J M, Faulkner J K, Wood B A, Darragh A, Lambe R F
J Antimicrob Chemother. 1986 Jun;17(6):801-9. doi: 10.1093/jac/17.6.801.
Following intravenous infusion of 800 mg of 14C-tinidazole during 30 min to two human subjects, a mean of 44% of the dose was excreted in urine during the first 24 h, increasing to 63% of the dose during five days: 12% of the dose was excreted in the faeces, indicating the possible involvement of biliary excretion and other secretory processes in the disposition of tinidazole. At 6 min after the end of the infusion, the mean plasma tinidazole concentration was 12 mg/l. Tinidazole was a major component in 0-120 h urine (about 32% of urinary 14C): the major metabolite in the 0-12 h urine examined was ethyl 2-(5-hydroxy-2-methyl-4-nitro-1-imidazolyl)ethyl sulphone (about 30% urinary 14C), the product of hydroxylation and nitro-group migration. These compounds were also present in the faeces. A minor urinary metabolite was 2-hydroxymethyltinidazole (about 9% urinary 14C), which was also present in plasma. The mean pharmacokinetic parameters obtained for tinidazole were similar to those reported in the literature; total clearance 51 ml/min, renal clearance 10 ml/min, volume of distribution 501 and half-life 11.6 h.
在30分钟内给两名受试者静脉输注800毫克14C-替硝唑后，在前24小时内，平均44%的剂量经尿液排出，5天内增加到剂量的63%；12%的剂量经粪便排出，这表明替硝唑的处置过程中可能涉及胆汁排泄和其他分泌过程。输注结束后6分钟，血浆替硝唑平均浓度为12毫克/升。替硝唑是0至120小时尿液中的主要成分（约占尿液中14C的32%）：在检测的0至12小时尿液中，主要代谢产物是2-(5-羟基-2-甲基-4-硝基-1-咪唑基)乙基砜乙酯（约占尿液中14C的30%），即羟基化和硝基迁移的产物。这些化合物也存在于粪便中。一种次要的尿液代谢产物是2-羟甲基替硝唑（约占尿液中14C的9%），其也存在于血浆中。替硝唑获得的平均药代动力学参数与文献报道的相似；总清除率51毫升/分钟，肾清除率10毫升/分钟，分布容积501，半衰期11.6小时。
