摘要
本文研究交链的甲氨蝶呤明胶微球(MTX-ms),经动物肝动脉栓塞后的体内药动学过程和微球在体内的生物降解期限等。肝动脉灌注MTX-ms后,外周血液中MTX血药浓度上升与下降缓慢,而灌注MTX溶液立即出现峰值并迅速下降;微球药物消除半衰期为MTX溶液的2.14倍,在16h的体内检测中,肝静脉局部的MTX-ms血药浓度始终高于MTX溶液组。经肝动脉造影随访证实,微球属血管末梢栓塞剂,明胶微球在体内降解时间约一月。微球栓塞后对肿瘤血供的切断以及药物在局部缓释作用对肝癌治疗是有积极意义的。
The cross-linked MTX-gelatin microsphere was chosen as an experimental model. Pharmacokinetics and biodegradable period of the microsphere were studied after hepatic arterial emblization in vivo in dogs.After hepatic arterial infusion, the concentration of MTX-ms in peripheral vein blood increased rapidly and declined slowly. In contrast, the peak time of the drug concentration of infused MTX solution appeared at once and decreased rapidly. The half-life of MTX-ms in vivo was 2.14 times as much as that of MTX solution. During the assay period of sixteen hours the drug concentration of MTX-ms in hepatic vein blood was constantly higher than that of MTX solution.The follow-up angiography revealed that microsphere is a kind of peripheral embolic agent and its degradable time in vivo is about one month.Both sustained release and embolization effecttiveness of microsphere will be significant in treatment of hepatic cancer.
出处
《药学学报》
CAS
CSCD
北大核心
1991年第2期139-143,共5页
Acta Pharmaceutica Sinica
关键词
靶向给药系统
甲氨喋呤
肝动脉栓塞
Gelatin-microsphere
Methotraxate
Hepatic arterial embolization
Pharmacokinetics
Sutained release
Targeting drug delivery system
