Healy D P, Sahai J V, Sterling L P, Racht E M
Department of Pharmacy and Pharmaceutics, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0581.
Antimicrob Agents Chemother. 1989 Nov;33(11):1994-7. doi: 10.1128/AAC.33.11.1994.
Interaction studies in dogs have indicated that antacids significantly decrease the oral bioavailability of cefixime. Twelve healthy adult male volunteers participated in a randomized, four-way crossover trial to evaluate the influence of an aluminum-magnesium antacid (Maalox; 20 ml) on the pharmacokinetics of cefixime (400 mg). Regimens were (i) cefixime alone; (ii) cefixime simultaneous with antacid; (iii) cefixime 2 h before antacid; and (iv) cefixime 2 h after antacid. Serial blood and urine samples were collected over a 24-h period following each dose of cefixime. There was a 1-week washout interval between regimens. Cefixime concentrations in serum and urine were analyzed by high-performance liquid chromatography. Maximum cefixime concentrations in serum for regimens i through iv were (mean +/- standard deviation) 4.9 +/- 1.4, 5.7 +/- 1.3, 5.1 +/- 1.0, and 5.5 +/- 1.5 micrograms/ml, respectively. Corresponding values for area under the serum concentration-time curve extrapolated to infinity were 38.3 +/- 14.5, 42.8 +/- 13.9, 38.5 +/- 9.8, and 41.6 +/- 16.7 micrograms.h/ml. There was a trend toward increased concentrations in serum and area under the curve of cefixime when it was administered concomitantly with antacid; however, these differences were not statistically significant (P greater than 0.05; analysis of variance). We conclude that single-dose administration of an aluminum-magnesium antacid does not significantly decrease the oral bioavailability of cefixime.
在犬类身上进行的相互作用研究表明,抗酸剂会显著降低头孢克肟的口服生物利用度。12名健康成年男性志愿者参与了一项随机、四交叉试验,以评估铝镁抗酸剂(胃得乐;20毫升)对头孢克肟(400毫克)药代动力学的影响。给药方案为:(i)单独使用头孢克肟;(ii)头孢克肟与抗酸剂同时服用;(iii)在服用抗酸剂前2小时服用头孢克肟;(iv)在服用抗酸剂后2小时服用头孢克肟。在每次服用头孢克肟后的24小时内采集系列血液和尿液样本。各给药方案之间有1周的洗脱期。血清和尿液中的头孢克肟浓度通过高效液相色谱法进行分析。方案i至iv血清中头孢克肟的最大浓度(均值±标准差)分别为4.9±1.4、5.7±1.3、5.1±1.0和5.5±1.5微克/毫升。血清浓度-时间曲线外推至无穷大时的相应面积值分别为38.3±14.5、42.8±13.9、38.5±9.8和41.6±16.7微克·小时/毫升。当头孢克肟与抗酸剂同时给药时,血清浓度和曲线下面积有升高的趋势;然而,这些差异无统计学意义(P>0.05;方差分析)。我们得出结论,单剂量服用铝镁抗酸剂不会显著降低头孢克肟的口服生物利用度。