【摘要】 本文建立了用反相高效液相色谱法测定丙硫苯咪唑及其代谢物丙硫苯咪唑亚砜、丙硫苯咪唑砜的血药浓度的方法,并测定了6头健康猪口服丙硫苯咪唑(25mg/kg)后亚砜和砜的血药浓度及有关药代动力学参数。结果:给药后20min采血,6头猪血中,丙硫苯咪唑原形药均未检出,而以丙硫苯咪唑亚砜和丙硫苯咪唑砜的形式出现。以NaVa pack C18 4μm 0.39×15cm为固定相,紫外检测器波长为290nm,甲苯咪唑为内标物,测定丙硫苯咪唑亚砜和砜.本法测得血清中亚砜的最低含量为23.56ng/mL,砜为16.54ng/mL。亚砜平均回收率为93.73±6.75％,砜为90.044±5.33％,不同浓度水平测定结果的日内和日间变动系数均在10％以下。丙硫苯咪唑亚砜和砜的药代动力学符合有吸收因素二室模型,健康猪口服丙硫苯咪唑后,亚砜半衰期(t1/B)为12.6466±1.8491h;血浆清除率(CL_B)为0.1364±0.0921L/(kg·h);血药浓度达峰时间(Tmax)为10h,峰浓度(Cmax)为11.919±1.382μg/mL血清;药时曲线下面积(AUC)为1156.69±742.52μg/(mL·h)。更多还原

【Abstract】 A RP-HPLC method assay of albendazole and its inter-mediates, sulfone and sulfoxide, in serum was established. Alben-dazole at dosage of 50 mg/kg was given orally to 6 healthy pigs, andthen its concentration in serum and the pharmacokinetic parameterswere determined. None of albendazole but sulfoxide and sulfonewas found in serum at 20 minutes after administration. Lowestconcentrations of sulfoxide and sulfone in serum are 0.02 ng/mLand 0.003 ng/mL respectively. After a single oral dose of 25 mg/kgto healthy pigs with albendazole, the pharmacokinetic parametersare as follows: t1/2β = 12.6466±1.8491 （h）; t1/2α= 4.6201±1.2186（h）;t1/2_Ka = 3.004±0. 1002 （h）; CL_B = 0. 1364±0.0921 （L/kg·h）; Ka = 0.2543±0.0606 （h）; Tmax （tp） = 10 （h）; Cmax= 11.919±1.382 （μg/mL）;AUC = 1156.69±742.52 [μg/（mL·h）].更多还原