Goldfarb J, Wormser G P, Inchiosa M A, Guideri G, Diaz M, Gandhi R, Goltzman C, Mascia A V
J Clin Pharmacol. 1986 Mar;26(3):222-6. doi: 10.1002/j.1552-4604.1986.tb02938.x.
The single-dose pharmacokinetics of oral ciprofloxacin were studied in ten patients with cystic fibrosis aged 18 to 34 years. Each patient received three different drug doses (500 mg, 750 mg, and 1,000 mg) at successive one-week intervals. Dosing and drug assays were double blinded. Blood and urine were assayed over the 48 hours following each dose. Ciprofloxacin was absorbed from the gastrointestinal tract. Peak serum concentrations averaged 2.8, 4.5, and 4.6 micrograms/mL respectively at the three doses, well above the mean inhibitory concentrations of most isolates of Pseudomonas aeruginosa. Time to peak concentration was approximately two hours. The range of sputum levels in three patients was 1.1-2.1 micrograms/mL at four hours after the three doses. The serum elimination half-life was 3.7 hours and was independent of dose. Urinary recovery was 26%; greater than 90% of urinary excretion occurred within the first 12 hours. The results of this study indicate that ciprofloxacin has potential for use in the treatment of P aeruginosa infections in patients with cystic fibrosis.
对10名年龄在18至34岁的囊性纤维化患者进行了口服环丙沙星的单剂量药代动力学研究。每位患者在连续一周的间隔内接受三种不同的药物剂量（500毫克、750毫克和1000毫克）。给药和药物检测采用双盲法。在每次给药后的48小时内对血液和尿液进行检测。环丙沙星从胃肠道吸收。三种剂量下的血清峰值浓度分别平均为2.8、4.5和4.6微克/毫升，远高于大多数铜绿假单胞菌分离株的平均抑制浓度。达到峰值浓度的时间约为两小时。三名患者在三种剂量给药后四小时的痰液水平范围为1.1 - 2.1微克/毫升。血清消除半衰期为3.7小时，且与剂量无关。尿液回收率为26%；超过90%的尿液排泄发生在最初12小时内。本研究结果表明，环丙沙星有潜力用于治疗囊性纤维化患者的铜绿假单胞菌感染。
