Davis R L, Koup J R, Williams-Warren J, Weber A, Smith A L
Antimicrob Agents Chemother. 1985 Jul;28(1):74-7. doi: 10.1128/AAC.28.1.74.
We compared the absorption of three formulations of ciprofloxacin after oral administration in 18 normal adult male volunteers. Each subject received 500 mg of ciprofloxacin as two 250-mg tablets, one 500-mg tablet, or a solution in a randomized crossover sequence. Pharmacokinetic parameters were determined by model independent methods. Because a solution is considered to be the ideal oral dosage form, the results determined for the tablets were compared to those for the solution. Mean values for the maximum concentration of drug in serum, the time to maximum concentration of drug in serum, and the elimination half-life were 3.23 micrograms/ml, 1.00 h, and 5.04 h, respectively, for the solution. The mean renal clearance of ciprofloxacin was 372 ml/min and accounted for at least 50% of the total clearance. We recovered 44.4, 48.6, and 55.8% of the administered ciprofloxacin from the urine as unchanged drug within 24 h after dosing with the 250-mg tablets, 500-mg tablets, or solution, respectively. The 500-mg tablets were found to be bioequivalent to the solution with regard to all pharmacokinetic parameters. The 250-mg tablet was not bioequivalent to either of the other formulations; the relative bioavailability values were 78.7 and 74.1%, respectively, for the 500-mg tablet and the solution. The clinical significance of this difference in bioavailability is yet to be determined.
我们比较了18名正常成年男性志愿者口服三种环丙沙星制剂后的吸收情况。每位受试者按随机交叉顺序分别服用500毫克环丙沙星，剂型分别为两片250毫克片剂、一片500毫克片剂或溶液剂。药代动力学参数通过非模型依赖方法测定。由于溶液剂被认为是理想的口服剂型，因此将片剂的测定结果与溶液剂的结果进行比较。溶液剂的血清药物最高浓度、血清药物达峰时间和消除半衰期的平均值分别为3.23微克/毫升、1.00小时和5.04小时。环丙沙星的平均肾清除率为372毫升/分钟，至少占总清除率的50%。服用250毫克片剂、500毫克片剂或溶液剂后，在给药后24小时内，从尿液中回收的未变化的环丙沙星分别占给药量的44.4%、48.6%和55.8%。就所有药代动力学参数而言，发现500毫克片剂与溶液剂生物等效。250毫克片剂与其他两种剂型均无生物等效性；500毫克片剂和溶液剂的相对生物利用度值分别为78.7%和74.1%。这种生物利用度差异的临床意义尚待确定。
