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目的采用尿药法进行去甲斑蝥素人体药动学研究。方法健康志愿者口服去甲斑蝥素片10mg后,收集尿样,经0.22μm微孔滤膜过滤,直接进样,采用C18色谱柱分离,梯度洗脱,多反应检测(MRM)方式检测m/z169.3→123.1的去甲斑蝥素特征碎片离子,尿药排泄速率法和亏量法计算去甲斑蝥素药动学参数。结果2种方法计算去甲斑蝥素健康志愿者体内消除半衰期t1/2为(4.01±0.91)和(3.56±0.96)h,24h内尿中去甲斑蝥素累积排泄率为(19.91±9.26)%。结论尿药法估算去甲斑蝥素人体药动学参数取样方便,样本处理简单。
Objective To study the pharmacokinetics of norcantharidin by urinary method. Methods Healthy volunteers were treated with 10 mg norcantharidin tablets. Urine samples were collected and filtered through a 0.22 μm microporous membrane filter. The samples were directly injected and separated on a C18 column by gradient elution. Multiple reaction detection (MRM) nocetanin characteristic fragment ions from z169.3 → 123.1, urinary drug excretion rate method, and deficit method were used to calculate the pharmacokinetic parameters of norcantharidin. Results The half-life (t1 / 2) of nornicotine in volunteers was (4.01 ± 0.91) and (3.56 ± 0.96) h, respectively, and the urinary norcantharidin excretion rate was (19.91 ± 9.26)% . Conclusion Urine method to estimate norcantharidin human pharmacokinetic parameters of sampling convenience, sample processing simple.