Weber H, Amlacher R, Preiss R, Hoffmann H
Institut für Mikrobiologie und Experimentelle Therapie, Jena.
Pharmazie. 1991 Aug;46(8):589-91.
The pharmacokinetics of bendamustine, (1; Cytostasan), an alkylating antineoplastic agent of the N-lost group, was investigated in B6D2F1 mice. After i.v. injection of the maximally tolerated dose of 50 mg/kg a rapid decrease of the unchanged drug in plasma (MRT 21.9 min) and slowly decreasing levels of mono-, dihydroxy and beta-hydroxy-1 were observed. Variations of the age of the animals as well as of the dose administered did not alter the short MRT of 1. 1 is excreted via the kidneys to a considerable extent showing a similar metabolite pattern in urine as in plasma. The absorption of the drug from the gastrointestinal tract is incomplete resulting in an absolute bioavailability of about 40%.
对N-失活基团的烷基化抗肿瘤药苯达莫司汀(1;商品名:瘤可然)在B6D2F1小鼠体内的药代动力学进行了研究。静脉注射最大耐受剂量50mg/kg后,观察到血浆中未变化药物迅速减少(平均驻留时间21.9分钟),单羟基、二羟基和β-羟基-1的水平缓慢下降。动物年龄以及给药剂量的变化并未改变1的短平均驻留时间。1在很大程度上经肾脏排泄,尿液中的代谢物模式与血浆中的相似。该药物从胃肠道的吸收不完全,绝对生物利用度约为40%。