用尿药法研究去甲斑蝥素人体药动学

Pharmacokinetics of Norcantharidin in Human by Urinary Excretion Method

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 pharmacokinetics of norcantharidin in human by urinary excretion method. METHODS The urine samples of healthy volunteers were collected after an oral administration of 10 mg norcantharidin tablets. The samples were filtered by 0.22μm film. The separation was performed on a C18 column （4.6 mm×250 mm, 5μm） with gradient elution. The fragment ion of m/z 169.3→123.1 was monitered by MRM mode. The pharmacokinetic parameters were calculated by urine elimination rate method and deficiency method. RESULTS The t1/2 of norcantharidin in healthy volunteers calculated by two methods were （4.01±0.91） and （3.56±0.96） h, respectively. The accumulate elimination percent of norcantharidin in urine was （19.91±9.26）% of the dose in 24 h. CONCLUSION It＇s suitable to estimate the pharmacokinetic parameters by urinary excretion method, with the merits of convenient sample collection and simply specimen disposal.