Chen R R, Lee T Y, Hsieh W C
School of Pharmacy, College of Medicine, National Taiwan University, Taipei, R.O.C.
J Formos Med Assoc. 1992 Dec;91(12):1177-81.
The effect of food on the pharmacokinetics of cefuroxime axetil was studied. Twelve healthy male subjects were included in this study. They were given single oral 500 mg doses of cefuroxime axetil alone or with food based on a balanced two-way crossover design. Plasma cefuroxime concentrations were assayed by the high performance liquid chromatographic method. When the drug was given alone, the area under the curve (AUC) was 15.77 +/- 4.12 mgh/L, Cmax was 4.20 +/- 1.05 mg/L, Tmax was 2.36 +/- 0.84 h, T1/2 was 1.56 +/- 0.26 h, and Clp/F was 34.13 +/- 10.39 L/h; 45.12 +/- 9.59% of the dose was recovered in the urine within 24 hours, and the renal clearance was 12.58 +/- 4.41 L/h. When the drug was given with food, the corresponding AUC was 23.46 +/- 4.57 mgh/L, Cmax was 7.10 +/- 1.41 mg/L, Tmax was 2.04 +/- 1.32 h, T1/2 was 1.40 +/- 0.23 h, and Clp/F was 21.93 +/- 5.18 L/h; the 24-hour urinary recovery was 69.33 +/- 6.13% and the renal clearance was 12.58 +/- 2.99 L/h. The above pharmacokinetic parameters obtained from the two regimens were compared by two-way ANOVA corrected for the change-over effect. No significant difference was found for Tmax, T1/2 or renal clearance (p > 0.05). Higher AUC, Cmax, urinary recovery and lower Clp/F values were observed for the regimen with food (p < 0.05). The plasma drug concentrations resulting from the regimen with food were higher throughout the 12-hour sampling period when compared to the regimen without food.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了食物对头孢呋辛酯药代动力学的影响。本研究纳入了12名健康男性受试者。基于平衡的双向交叉设计，他们单独口服500mg剂量的头孢呋辛酯或与食物一起服用。采用高效液相色谱法测定血浆头孢呋辛浓度。单独给药时，曲线下面积（AUC）为15.77±4.12mgh/L，Cmax为4.20±1.05mg/L，Tmax为2.36±0.84h，T1/2为1.56±0.26h，Clp/F为34.13±10.39L/h；24小时内45.12±9.59%的剂量在尿液中回收，肾清除率为12.58±4.41L/h。与食物一起给药时，相应的AUC为23.46±4.57mgh/L，Cmax为7.10±1.4mg/L，Tmax为2.04±1.32h，T1/2为1.40±0.23h，Clp/F为21.93±5.18L/h；24小时尿液回收率为69.33±6.13%，肾清除率为12.58±2.99L/h。通过校正交叉效应的双向方差分析比较了两种给药方案获得的上述药代动力学参数。Tmax、T1/2或肾清除率无显著差异（p>0.05）。食物给药方案的AUC、Cmax、尿液回收率更高，Clp/F值更低（p<0.05）。与无食物给药方案相比，食物给药方案在12小时采样期内产生的血浆药物浓度更高。（摘要截断于250字）
