Verho M, Malerczyk V, Grötsch H, Lorenz H
Clinical Research Department, Hoechst AG, Frankfurt, FRG.
Drugs Exp Clin Res. 1988;14(8):539-45.
An open placebo-controlled study on eleven healthy male volunteers was carried out to investigate renal tolerance and the possibility of crystalluria after oral and intravenous administration of ofloxacin. Subjects received single doses of 200 and 400 mg ofloxacin orally, 200 mg ofloxacin intravenously, or placebo. Urine was collected in several fractions on each study day and the urine volume, excretion of ofloxacin, and excretion of creatinine, alanine aminopeptidase, N-acetyl-beta-D-glucosaminidase, and gamma-glutamyltransferase were calculated in each fraction collected. Furthermore, the urine was investigated microscopically to determine whether ofloxacin crystals were present. Serum creatinine and creatinine clearance were also calculated. No relevant changes in creatinine clearance were observed and no drug crystals were found in the urine which indicates that renal tolerance was good. There were no differences in ofloxacin recovery after oral or intravenous administration, confirming that absolute bioavailability of the oral form is excellent.
对11名健康男性志愿者进行了一项开放的安慰剂对照研究，以调查口服和静脉注射氧氟沙星后的肾脏耐受性及出现结晶尿的可能性。受试者分别口服200毫克和400毫克氧氟沙星、静脉注射200毫克氧氟沙星或服用安慰剂。在每个研究日分多次收集尿液，并计算每次收集的尿液样本的尿量、氧氟沙星排泄量以及肌酐、丙氨酸氨基肽酶、N-乙酰-β-D-氨基葡萄糖苷酶和γ-谷氨酰转移酶的排泄量。此外，对尿液进行显微镜检查以确定是否存在氧氟沙星晶体。还计算了血清肌酐和肌酐清除率。未观察到肌酐清除率有相关变化，且尿液中未发现药物晶体，这表明肾脏耐受性良好。口服或静脉给药后氧氟沙星的回收率没有差异，证实口服剂型的绝对生物利用度极佳。
