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用微生物测定法对环丙沙星３种剂型在６２名男性健康志愿者身上进行药物动力学研究。在１６名受试者静滴环丙沙星注射液（２００ｍｇ／１００ｍｌ）后，０、１、４、１２ｈ的血药浓度分别为３．６８±０．６３、≤１、０．３３～０．４３及０．１μｇ／ｍｌ，药动学参数Ｔ１／２为３．２４ｈ，总清除率３９３．５ｍｌ／ｍｉｎ，ＡＵＣ０～２４６．２１ｈ·μｇ／ｍｌ，Ｖｓｓ１５５．０±３４．２Ｌ。单次口服环丙沙星１００及５００ｍｇ，体内平均药动学参数Ｃｍａｘ分别为２．３１±０．２８及２．４９±０．２４μｇ／ｍｌ，Ｔｍａｘ分别为１．２６±０．１８及１．４７±０．２１ｈ，Ｔ１／２为２．６９±０．４８及３．８７±０．５３ｈ，ＡＵＣ０～２４为１２．８１±０．８５及１５．０２±２．１１ｈ·μｇ／ｍｌ，结果与文献报道相同。此外，对静滴及口服两种给药途径的血药浓度与临床疗效关系以及统计矩法与房室模型在药物动力学研究中的选用进行了讨论。
Pharmacokinetic studies were conducted on 62 male healthy volunteers using the microbiological assay for three formulations of ciprofloxacin. After intravenous infusion of ciprofloxacin (200mg / 100ml) in 16 subjects, the plasma concentrations at 0, 1, 4 and 12h were 3.68 ± 0.63 and 1, 0.33 and 0 .43 and 0.1μg / ml, the pharmacokinetic parameters T1 / 2 was 3.24h, the total clearance rate was 393.5ml / min, AUC0 ~ 246.21h · μg / ml, Vss155.0 ± 34.2L. The single oral ciprofloxacin 100 and 500mg, the average pharmacokinetic parameters Cmax were 2.31 ± 0.28 and 2.49 ± 0.24μg / ml, Tmax were 1.26 ± 0.18 and 1 .47 ± 0.21h, T1 / 2 was 2.69 ± 0.48 and 3.87 ± 0.53h, AUC0 ~ 24 was 12.81 ± 0.85 and 15.02 ± 2.11h · μg / ml The results are the same as reported in the literature. In addition, the relationship between plasma concentration and clinical efficacy of both intravenous and oral routes of administration and the use of statistical moment method and atrioventricular model in pharmacokinetic studies are discussed.