Kearns G L, Abdel-Rahman S M, Jacobs R F, Wells T G, Borin M T
Section of Pediatric Clinical Pharmacology and Experimental Therapeutics, The Children's Mercy Hospital, Kansas City, MO 64108, USA.
Pediatr Infect Dis J. 1998 Sep;17(9):799-804. doi: 10.1097/00006454-199809000-00010.
Cefpodoxime, an oral third generation cephalosporin antibiotic, is used for the treatment of acute upper respiratory tract infection caused by susceptible bacteria in children 5 months to 12 years of age. We report the results of a randomized two-way crossover study designed to characterize the disposition of a single dose (10 mg/kg) of cefpodoxime proxetil oral suspension in children, under fed and fasted conditions.
Seventeen children (8.4 months to 12.2 years old, seven female) participated in this study. Each subject received a single 10-mg/kg dose of cefpodoxime proxetil oral suspension, after a predose fast and again coadministered with food. Repeated blood samples (n=10) were obtained during 12 h postdose and cefpodoxime was quantified from plasma by high performance liquid chromatography. Plasma concentration vs. time data were curve fit for each subject with a nonlinear weighted least squares algorithm, and pharmacokinetic parameters were determined from the polyexponential estimates.
Cefpodoxime disposition was best characterized using a one-compartment open model with first order absorption. The area under the plasma concentration vs. time curve, Cmax and Ke were not significantly different between fed and fasted conditions. However, Tmax was significantly prolonged (fed=2.79+/-1.10 h vs. fasted=1.93+/-0.54 h) and Ka was significantly smaller (fed=0.42+/-0.14 h(-1) vs. fasted=0.81+/-0.72 h(-1)) in the fed state.
Administration of cefpodoxime in the presence of food affected the rate but not the extent of absorption. Cefpodoxime proxetil oral suspension can be administered without regard to meals in children 6 months to 12 years of age.
头孢泊肟酯是一种口服第三代头孢菌素抗生素,用于治疗5个月至12岁儿童由易感细菌引起的急性上呼吸道感染。我们报告了一项随机双向交叉研究的结果,该研究旨在确定在进食和空腹条件下,儿童单次口服(10mg/kg)头孢泊肟酯干混悬剂的处置情况。
17名儿童(年龄8.4个月至12.2岁,7名女性)参与了本研究。每位受试者在给药前禁食后接受单次10mg/kg剂量的头孢泊肟酯干混悬剂,之后再次与食物同服。给药后12小时内重复采集血样(n=10),采用高效液相色谱法对血浆中的头孢泊肟进行定量。使用非线性加权最小二乘法算法对每位受试者的血浆浓度-时间数据进行曲线拟合,并从多指数估计值中确定药代动力学参数。
头孢泊肟的处置情况以具有一级吸收的单室开放模型最为合适。进食和空腹条件下,血浆浓度-时间曲线下面积、Cmax和Ke无显著差异。然而,进食状态下Tmax显著延长(进食=2.79±1.10小时,空腹=1.93±0.54小时),Ka显著减小(进食=0.42±0.14h-1,空腹=0.81±0.72h-1)。
进食时服用头孢泊肟影响吸收速率,但不影响吸收程度。6个月至12岁儿童服用头孢泊肟酯干混悬剂时无需考虑用餐情况。