Okuno A, Taguchi T, Inyaku F, Yano K, Suzuki Y
Pediatr Pharmacol (New York). 1983;3(1):43-7.
Pharmacokinetics of propylthiouracil after a single oral dose were studied in six pediatric patients with Graves disease, with respect to influence of food intake. Propylthiouracil administration in the fasting state induced a rapid rise of plasma level reaching a peak of 30 to 60 min. Peak values ranged from 7.2 to 18 micrograms/ml with administered dose (100 to 280 mg/m2 BSA) and plasma half-life was 1.3 +/- 0.41 hr (mean +/- SD). Single compartment model with first order absorption showed excellent fit to the data obtained in the fasting state, but not in the fed state. Most individuals showed marked difference in the pattern of propylthiouracil concentration-time curves between the fasting and the fed state. Food intake prior to the drug ingestion was associated with lower and delayed peak and variable AUC values. These results indicate that propylthiouracil administration in the fasting state is more advisable for obtaining a consistent bioavailability.
在六名患有格雷夫斯病的儿科患者中，研究了单次口服丙硫氧嘧啶后的药代动力学，探讨了食物摄入的影响。在禁食状态下给予丙硫氧嘧啶会导致血浆水平迅速上升，在30至60分钟达到峰值。峰值浓度范围为7.2至18微克/毫升，给药剂量为（100至280毫克/平方米体表面积），血浆半衰期为1.3±0.41小时（平均值±标准差）。具有一级吸收的单室模型对禁食状态下获得的数据拟合良好，但对进食状态下的数据拟合不佳。大多数个体在禁食和进食状态下丙硫氧嘧啶浓度-时间曲线模式存在明显差异。服药前摄入食物会导致峰值降低且延迟出现，AUC值也会有所变化。这些结果表明，为获得一致的生物利用度，禁食状态下服用丙硫氧嘧啶更为可取。
