【摘要】 应用高效液相色谱法建立了测定人体血清中丙硫咪唑(Albendazole)及主要代谢产物砜(Sulphone)和亚砜(Sulphoxide)的分析方法。本方法选用硅胶色谱柱,正已烷、氯仿、甲醇为流动相,检测波长292nm,甲苯咪唑(Mebendazole)为内标物,醋酸乙酯为提取剂,测定了12例肝包虫病患者血药浓度。该方法分离良好,峰形锐尖,13分钟内可完成分析。丙硫咪唑、砜和亚砜检出限分别为25、25和50(ng/ml),变异系数小于5.79％,回收率101-5±6 .96％。测定结果提示丙硫咪唑在人体内易氧化分解,大部分转化为亚砜,亚砜的血清浓度最高值出现在连续服药后第48小时,停药3天后该药物及主要代谢产物从血中基本清除。结合临床、B超和病理观察,病人血中丙硫咪唑亚砜浓度值高者治疗效果显著,提示增大用药剂量有临床治疗意义。更多还原

【Abstract】 The authors analysed, Albendazole (ABZ) and its active metabolites, sulphone and sulphoxide in human serum by applying high performance liquid chromatography (HPLC). The samples were extracted with ethylacetate which contained Mebendazole (MBZ) as an internal standard. Analytical column was ZORBAX SIL (5-6u) 250×4.6mm (ID). The mobile phase was composed of hexame/chlaform/methanol. The monitoring wave was at 292nm. The detection limit was 50 ng/ml for sulphoxide and 25 ng/ml for ABZ and sttlphone. The coefficent variation was lower than 5.79% and the relative recovery 101.54±6.96％ for ABZ sulphone and sulphoxide. The results indicated that the highest concentration of sulphoxide (1838ng/ml) was monitored at 48 hour after taking ABZ and eliminated in 72 hours after taken it from the serum. Comparied with 10-14 mg/kg/d dose, we obtained the higher concentration of sulphoxide with 20 mg/kg/d dose in the serum. It indicates that there is clinical significance wher we increase the dose in the treatment of echinococcosis.更多还原