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作者报道了动物(鼠)口服脂质体阿苯达唑后血浆、肝脏、包虫囊组织和囊液中阿苯达唑及主要代谢产物阿苯达唑砜和阿苯达唑亚砜的反相HPLC法。同时进行了药物动力学研究和并用西咪替丁后对血、肝药物浓度的影响。结果表明,阿苯达唑在血浆、囊液中的检出限为0.05μg/ml,在肝脏和囊组织中为0.10μg/g;砜和亚砜在血浆、囊液中均为0.01μg/ml,在肝脏和囊组织中均为0.02μg/g。药物动力学结果显示,阿苯达唑脂质体、混悬液及脂质体并用西咪替丁后的体内过程均符合二室模型,混悬液并用西咪替丁后符合单室模型。阿苯达唑脂质体具有一定的缓释及靶向的作用,西咪替丁可能增强阿苯达唑的缓释作用,同时可能加速阿苯达唑亚砜的代谢。
The authors reported the effects of albendazole and major metabolites albendazole sulfoxide and albendazole sulfoxide in plasma, liver, hydatid cyst tissue and cystic fluid after oral administration of albendazole to animals (rats) Phase HPLC method. Simultaneous pharmacokinetic studies and the effect of cimetidine on blood and liver drug concentrations were also studied. The results showed that the detection limit of albendazole in plasma and cystic fluid was0.05μg / ml, and in the liver and cystic tissue was0.10μg / g; the contents of sulfone and sulfoxide in plasma and cystic fluid were0.01μg / ml, 0.02μg / g in liver and cyst tissues. Pharmacokinetic results showed that the in vivo process of albendazole liposomes, suspensions and liposomes with cimetidine were in accordance with the two-compartment model. The suspension and cimetidine were consistent with the single-compartment model. Albendazole liposomes have a certain degree of sustained release and targeted effects, cimetidine may enhance the sustained release of albendazole, at the same time may accelerate the metabolism of albendazole sulfoxide.