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阿苯达唑(Albendazole,ABZ)是一种广谱抗寄生虫药,它在宿主体内极易被代谢为阿苯达唑亚砜(Albendazole suLfoxide,SX)和阿苯达唑砜(Albenda-zole sulphone,SN),且前者经过体内试验证明有抗细粒棘球蚴病的作用.为了使药物具有定向性和在靶区(肝脏包虫组织)具有滞留性以及达到缓释的目的,我们将ABZ制成脂质体,建立了动物(鼠)口服ABZ脂质体后测定血浆、肝脏、包虫囊液及囊组织中的ABZ及主要代谢产物SX和SN的反相HPLC法。同时进行了药代动力学研究以及并用西咪替丁后对血、肝药物浓度的影响。采用Neceleosil C_(13)柱,以甲醇:乙腈:水(5:37:58)为流动相,292 nm为检测波长,甲苯达唑为内标,样品提取溶剂为醋酸乙酯。结
Albendazole (ABZ) is a broad-spectrum antiparasitic agent that is easily metabolized in the host body to Albendazole sulfoxide (SX) and Albendazole-sulfone sulphone, SN), and the former is proved to have the anti-granulomatosis effect through in vivo experiments.In order to make the drug have the orientation and retain the target area (liver hydatid tissue) and achieve the purpose of sustained release, we will ABZ liposomes were established, and the ABZ liposomes were established after oral administration of ABZ liposomes, and the reverse phase HPLC method was established for the determination of ABZ and the major metabolites SX and SN in plasma, liver, hydatid fluid and cyst tissues. At the same time, the study of pharmacokinetics and the effect of cimetidine on blood and liver drug concentration were performed. Using Neceleosil C_ (13) column, methanol: acetonitrile: water (5:37:58) as the mobile phase, 292 nm as the detection wavelength, mebendazole as internal standard, the sample was extracted with ethyl acetate. Knot