Nix D E, Watson W A, Lener M E, Frost R W, Krol G, Goldstein H, Lettieri J, Schentag J J
School of Pharmacy, State University of New York, Buffalo.
Clin Pharmacol Ther. 1989 Dec;46(6):700-5. doi: 10.1038/clpt.1989.207.
The effect of an antacid (Maalox) and ranitidine administration on the absorption of ciprofloxacin was evaluated in healthy male volunteers who were enrolled in three separate studies. Each study was designed at a three- or four-period crossover and included the administration of 750 mg ciprofloxacin alone as a control treatment. Treatments that were evaluated included the administration of ciprofloxacin 5 to 10 minutes, 2 hours, 4 hours, and 6 hours after a single 30 ml dose of antacid; the administration of antacid 2 hours after ciprofloxacin was given; and the administration of ciprofloxacin 2 hours after a 200 mg ranitidine tablet. Administration of antacid within 4 hours before ciprofloxacin dose resulted in a significant decrease in ciprofloxacin absorption (p less than 0.05). Percentages of relative bioavailability compared with control values were 15.1%, 23.2%, and 70% for the 5 to 10 minute, 2 hour, and 4 hour antacid pretreatments, respectively. Administration of antacid 6 hours before or 2 hours after the ciprofloxacin dose did not affect absorption. Ranitidine did not alter ciprofloxacin absorption. Antacids that contain magnesium and aluminum salts may reduce the absorption of ciprofloxacin. The extent of this interaction appears to increase as the time between administration of the two drugs decreases. Ranitidine is suggested as an alternative to antacids for patients receiving treatment with ciprofloxacin.
在参加三项独立研究的健康男性志愿者中,评估了抗酸剂(氢氧化铝镁)和雷尼替丁给药对环丙沙星吸收的影响。每项研究设计为三周期或四周期交叉试验,包括单独给予750毫克环丙沙星作为对照治疗。评估的治疗方法包括在单次服用30毫升抗酸剂后5至10分钟、2小时、4小时和6小时给予环丙沙星;在给予环丙沙星2小时后给予抗酸剂;以及在服用200毫克雷尼替丁片后2小时给予环丙沙星。在环丙沙星给药前4小时内给予抗酸剂会导致环丙沙星吸收显著降低(p小于0.05)。与对照值相比,5至10分钟、2小时和4小时抗酸剂预处理的相对生物利用度百分比分别为15.1%、23.2%和70%。在环丙沙星给药前6小时或给药后2小时给予抗酸剂不影响吸收。雷尼替丁不改变环丙沙星的吸收。含有镁盐和铝盐的抗酸剂可能会降低环丙沙星的吸收。这种相互作用的程度似乎随着两种药物给药时间间隔的缩短而增加。对于接受环丙沙星治疗的患者,建议使用雷尼替丁替代抗酸剂。