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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。
A method for the determination of Albendazole and its major metabolites Sulphone and Sulphoxide in human serum was established by high performance liquid chromatography (HPLC). The method uses silica gel column, n-hexane, chloroform and methanol as the mobile phases, the detection wavelength is 292nm, mebendazole is the internal standard substance and ethyl acetate is the extractant, and the blood samples of 12 patients with hepatic hydatid disease concentration. The method is well separated, peak shape acute, 13 minutes to complete the analysis. The limits of detection of albendazole, sulfone and sulfoxide were 25, 25 and 50 (ng / ml), the coefficient of variation was less than 5.79% and the recoveries were 101-5 ± 6.96%. Measurement results suggest that albendazole in the human body easily oxidative decomposition, most of the conversion to sulfoxides, the highest serum concentrations of sulfoxides appear in the first 48 hours after taking the drug three days after stopping the drug and the main metabolites from the blood basic Clear. Combined with clinical, B ultrasound and pathological observation, the patients with high concentration of propylthiouracil sulfoxide treatment effect is significant, suggesting that increasing the dose of a clinical significance.