De Bernardis E, Bonaccorsi S, Carlino S, Picari M, Rizza V
Institute of Pharmacology, University of Catania School of Medicine, Italy.
Int J Clin Pharmacol Res. 1988;8(4):239-45.
The pharmacokinetics of ofloxacin was studied in normal male volunteers selected from a student population. The aim of this study was to ascertain whether ofloxacin accumulated in plasma after administering six oral doses of the drug. The drug was administered in 300 mg tablets at intervals of 12 h for a total period of 72 h. The results clearly demonstrated that a modest accumulation of ofloxacin was observed between the first and second oral intake of the drug (R = 1.4); thereafter a steady-state plasma concentration was maintained at all time periods tested during the study. Furthermore, there was a broad fluctuation of approximately 80% between the Cmax and Cmin in the plasma levels of the drug during a 12-hour dosing interval. Hence demonstrating that a constant dose, repeatedly administered at a constant time interval of 12 h, ensured a broad range of concentrations of ofloxacin plasma, bile and other tissues which should favour the therapeutic success of the drug. There was agreement between the results of these studies and those in hospitalized patients suffering from severe infections. Analysis of ofloxacin after multiple dosing regimens in these patients showed measurable concentrations of the drug in the various tissues examined; hence suggesting a relative good bioavailability of the drug, which presumably reflected the high degree of success rates in these patients.
在从学生群体中挑选出的正常男性志愿者身上研究了氧氟沙星的药代动力学。本研究的目的是确定在口服六剂该药物后，氧氟沙星是否会在血浆中蓄积。药物以300毫克片剂形式给药，间隔12小时，共给药72小时。结果清楚地表明，在首次和第二次口服该药物之间观察到氧氟沙星有适度的蓄积（R = 1.4）；此后，在研究期间测试的所有时间段内，血浆浓度均维持在稳态。此外，在12小时给药间隔期间，该药物血浆水平的Cmax和Cmin之间有大约80%的广泛波动。因此表明，以12小时的恒定时间间隔重复给予恒定剂量，可确保氧氟沙星在血浆、胆汁和其他组织中有广泛的浓度范围，这应有利于药物的治疗成功。这些研究结果与患有严重感染的住院患者的研究结果一致。对这些患者多次给药方案后的氧氟沙星分析表明，在检查的各种组织中均检测到该药物的可测量浓度；因此表明该药物具有相对良好的生物利用度，这大概反映了这些患者的高成功率。
