Lin C, Kumari P, Perrotta R J, Reidenberg B E
Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
Antimicrob Agents Chemother. 1996 Jun;40(6):1394-6. doi: 10.1128/AAC.40.6.1394.
The penetration of ceftibuten, an extended-spectrum oral cephalosporin, into middle ear fluid (MEF) was evaluated in pediatric patients during a course of daily oral doses of 9 mg/kg of body weight for 10 days. Plasma and MEF collected at 2, 4, 6, or 12 h after at least 3 days of dosing were analyzed for ceftibuten by a high-pressure liquid chromatography method, and the data were used to calculate pharmacokinetic parameters. Plasma and MEF had almost identical maximum concentrations (Cmax) of ceftibuten (14 micrograms/ml). These Cmax values in MEF during acute otitis media were well in excess of the MIC for 90% of the isolates of each of four major pathogens in this disease. The time to Cmax was longer in MEF (4 h) than in plasma (2 h). Excellent penetration (71%) of ceftibuten into MEF was observed on the basis of the area under the curve ratio (MEF/plasma). These data clearly indicate that ceftibuten penetrated well into the MEF to yield clinically effective concentrations.
在儿科患者中，评估了广谱口服头孢菌素头孢布烯在每日口服剂量为9 mg/kg体重、疗程为10天的情况下进入中耳液（MEF）的情况。在给药至少3天后的2、4、6或12小时采集血浆和MEF，采用高压液相色谱法分析其中的头孢布烯，并将数据用于计算药代动力学参数。血浆和MEF中头孢布烯的最大浓度（Cmax）几乎相同（14微克/毫升）。在急性中耳炎期间，MEF中的这些Cmax值远远超过了该疾病四种主要病原体中90%的分离株的最低抑菌浓度（MIC）。MEF达到Cmax的时间（4小时）比血浆（2小时）长。根据曲线下面积比（MEF/血浆），观察到头孢布烯对MEF具有良好的渗透性（71%）。这些数据清楚地表明，头孢布烯能很好地渗透到MEF中，产生临床有效浓度。
