Riccardi R, Balis F M, Ferrara P, Lasorella A, Poplack D G, Mastrangelo R
Division of Pediatric Oncology, Catholic University of Rome, Italy.
Pediatr Hematol Oncol. 1986;3(4):319-24. doi: 10.3109/08880018609031233.
Plasma levels of 6-mercaptopurine (6-MP) were measured after oral administration in 17 children with acute lymphoblastic leukemia (ALL). In the fasting state or after a breakfast consisting of 250 ml milk and 50 g biscuits, 6-MP was administered at a dose of 75 mg/m2. In patients studied in a fasting state, the mean time to plasma peak (tmax) level was 1.2 h, whereas in patient studied after breakfast the mean tmax was 2.3 h. This difference is statistically significant (p less than 0.001). Moreover, the 6-MP peak plasma concentration (cmax) and the areas under the plasma concentration time curves (AUC) were significantly reduced when the drug was administered after breakfast. The mean Cmax +/- SD were 0.98 +/- 0.54 microM and 0.63 +/- 0.48 microM, respectively (p less than 0.05). The mean 6-MP AUC +/- SD in patients studied in a fasting state and after breakfast were 143 +/- 69 microM min and 105 +/- 68 microM, respectively (p less than 0.01). These results indicated that 6-MP should be taken in a fasting state to optimize drug absorption in children undergoing chemotherapy for ALL.
对17名急性淋巴细胞白血病（ALL）患儿口服给药后测定了6-巯基嘌呤（6-MP）的血浆水平。在空腹状态下或进食由250毫升牛奶和50克饼干组成的早餐后，以75毫克/平方米的剂量给予6-MP。在空腹状态下研究的患者中，血浆达到峰值（tmax）水平的平均时间为1.2小时，而在早餐后研究的患者中，平均tmax为2.3小时。这种差异具有统计学意义（p小于0.001）。此外，早餐后给药时，6-MP的血浆峰值浓度（cmax）和血浆浓度-时间曲线下面积（AUC）显著降低。平均Cmax±SD分别为0.98±0.54微摩尔/升和0.63±0.48微摩尔/升（p小于0.05）。空腹状态下和早餐后研究的患者中，6-MP的平均AUC±SD分别为143±69微摩尔·分钟和105±68微摩尔（p小于0.01）。这些结果表明，接受ALL化疗的儿童应在空腹状态下服用6-MP，以优化药物吸收。
