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目的：为了解三氧化二砷经静脉用药在体内的药物代谢以及对人体的毒副作用。方法：用气相色谱法对８例用三氧化二砷静脉滴注治疗复发的急性早幼粒细胞白血病（ＡＰＬ）患者进行了药代动力学研究，同时监测了尿砷排泄及末梢砷蓄积情况。持续２小时静脉滴注１０ｍｇ三氧化二砷注射液，测得高峰血浓度Ｃｐｍａｘ为０．９４±０．３７ｍｇ／Ｌ，达峰时间Ｔｐｅａｋ为４小时，血浆浓度分布半衰期Ｔ１／２α为０．８９±０．２９小时，消除半衰期Ｔ１／２β为１２．１３±３．３１小时，系统清除率ＣＬｓ为１．４３±０．１７Ｌ／ｈ，表观分布容积Ｖｃ为３．８３±０．４５Ｌ，浓度－时间曲线下面积（ＡＵＣ）为７．２５±０．９７ｍｇ·ｈ／Ｌ。在持续用药过程中，药代动力学参数基本保持一致。疗程中，２４小时尿砷排泄量为每日给药量的１％～８％，末梢砷蓄积上升较明显，最高时可达用药前５～７倍。停药后尿砷排泄和末梢砷蓄积即开始逐步下降。结论：三氧化二砷是一种治疗ＡＰＬ相对安全而有效的药物，但在人体头发和指（趾）甲内存在一定的蓄积作用。
Objective: To understand the metabolism of arsenic trioxide in the body via intravenous drug and its toxic side effects on human body. Methods: Pharmacokinetic studies of 8 patients with acute promyelocytic leukemia (APL) treated with arsenic trioxide infusion were performed by gas chromatography. Urinary arsenic excretion and peripheral arsenic accumulation were monitored. Intravenous 10 mg arsenic trioxide injection was continued for 2 hours. The peak plasma concentration Cpmax was 0.94±0.37 mg/L, peak time Tpeak was 4 hours, and plasma concentration distribution half-life T1/2α was 0.89±0. At 29 hours, the elimination half-life T1/2β was 12.13±3.31 hours, the system clearance CLs was 1.43±0.17L/h, and the apparent volume of distribution Vc was 3.83±0.45L. Concentration-time The area under the curve (AUC) was 7.25±0.97 mg·h/L. In the course of continuous medication, the pharmacokinetic parameters remained basically the same. During the course of treatment, the 24-hour urine arsenic excretion amounted to 1% to 8% of the daily dose, and the accumulation of arsenic in the distal tip rose more markedly. The highest arsenic excretion was 5 to 7 times before administration. Urinary arsenic excretion and terminal arsenic accumulation began to gradually decline after drug withdrawal. Conclusion: Arsenic trioxide is a relatively safe and effective drug for the treatment of APL, but there is a certain accumulation in the human hair and nails.