Giachetti C, Bertolino M, Canali S, Lombardini E, Monzani M V, Sala A, Zanolo G
Istituto di Ricerche Biomediche A. Marxer, RBM S.p.A., Colleretto Giacosa (TO), Italy.
Eur J Drug Metab Pharmacokinet. 1998 Apr-Jun;23(2):239-50. doi: 10.1007/BF03189346.
Pharmacokinetics of [14C]-ITF-296 and its metabolites, ITF-1124 and ITF-1577, were studied in dogs and monkeys after a single intravenous (2.5 mg/kg) and oral (10 mg/kg) administration. Radioactivity was measured by LSC while unchanged drug and its metabolites in plasma were assayed by an HPLC-UV method. The absorption of [14C]-ITF-296 after oral administration is practically complete both in dogs and in monkeys. The determination of unchanged drug and its metabolites shows quite a similar profile in dogs and monkeys for ITF-296 and ITF-1124 and a different time-course for ITF-1577. Elimination of radioactivity occurs mainly in urine (namely 70-80%) for both species and the recovery of the dose (higher than 90%) takes place up to 96 h after both treatments.
在犬和猴单次静脉注射(2.5mg/kg)和口服(10mg/kg)[14C]-ITF-296及其代谢产物ITF-1124和ITF-1577后,对其药代动力学进行了研究。通过液体闪烁计数法测量放射性,同时采用高效液相色谱-紫外法测定血浆中未变化的药物及其代谢产物。口服给药后,犬和猴体内的[14C]-ITF-296吸收几乎完全。未变化药物及其代谢产物的测定结果显示,犬和猴体内ITF-296和ITF-1124的情况颇为相似,而ITF-1577的时间进程则有所不同。两种动物放射性的消除主要通过尿液(即70-80%),两种给药方式后96小时内剂量回收率均高于90%。