Ledergerber B, Bettex J D, Joos B, Flepp M, Lüthy R
Antimicrob Agents Chemother. 1985 Mar;27(3):350-2. doi: 10.1128/AAC.27.3.350.
Ciprofloxacin was administered to 10 volunteers, who received seven oral doses of 250 mg each at 12-h intervals. Volunteers alternately fasted (F) or received a standard breakfast (B) before the morning dose. Pharmacokinetic parameters were derived from high-pressure liquid chromatography data from samples taken after the first and seventh doses and were analyzed in addition for differences caused by food intake. A significant (P less than 0.05) influence of the standard breakfast on the time to the peak was observed. Peak levels (+/- standard deviation) after the first and seventh doses averaged F (fasting): 1.35 +/- 0.17, B (breakfast): 1.02 +/- 0.28 micrograms/ml, and F: 1.41 +/- 0.32, B: 1.17 +/- 0.5 micrograms/ml, respectively. Mean trough concentrations after the first and seventh doses were F: 0.10 +/- 0.03, B: 0.14 +/- 0.03 micrograms/ml, and F: 0.16 +/- 0.05, B: 0.14 +/- 0.04 microgram/ml, respectively. As with the peak, trough concentrations were not affected significantly by food intake or by accumulation over the study period. Breakfast equally did not affect the terminal half-lives, which averaged F: 3.97 +/- 0.67, B: 4.35 +/- 0.88 h after the first dose and F: 4.64 +/- 0.91, B: 3.72 +/- 0.84 h after the seventh dose. Twelve-hour urinary recovery measured by high-pressure liquid chromatography averaged F: 31, B: 30% for the first dose and, in spite of a possible carry-over from the sixth dose, decreased to F: 25, B: 28% after the seventh dosing interval. When measured by bioassay, an increase of urinary recovery between the first dose (F: 38, B: 38%) and the seventh dose (F: 45, B: 45%) was observed. These differences suggest induction of drug metabolism with repeated doses. Ciprofloxacin was well tolerated by the volunteers.
给10名志愿者服用环丙沙星，他们每隔12小时口服7次，每次250毫克。志愿者在早晨服药前交替禁食（F）或食用标准早餐（B）。药代动力学参数来自首次和第七次给药后采集样本的高压液相色谱数据，并分析了食物摄入造成的差异。观察到标准早餐对达峰时间有显著影响（P小于0.05）。首次和第七次给药后的峰浓度（±标准差）平均为：禁食（F）时，1.35±0.17；早餐（B）时，1.02±0.28微克/毫升，以及首次给药后禁食时1.41±0.32，早餐时1.17±0.5微克/毫升。首次和第七次给药后的平均谷浓度分别为：禁食时0.10±0.03，早餐时0.14±0.03微克/毫升，以及首次给药后禁食时0.16±0.05，早餐时0.14±0.04微克/毫升。与峰浓度一样，谷浓度不受食物摄入或研究期间蓄积的显著影响。早餐同样不影响终末半衰期，首次给药后平均禁食时为：3.97±0.67小时，早餐时为4.35±0.88小时；第七次给药后禁食时为4.64±0.91小时，早餐时为3.72±0.84小时。通过高压液相色谱法测得的12小时尿回收率，首次给药时平均禁食为31%，早餐为30%，尽管可能存在第六次给药的残留影响，但在第七次给药间隔后降至禁食时25%，早餐时28%。通过生物测定法测量时，观察到首次给药（禁食时38%，早餐时38%）和第七次给药（禁食时45%，早餐时45%）之间尿回收率有所增加。这些差异表明重复给药会诱导药物代谢。志愿者对环丙沙星耐受性良好。
