【摘要】 本文主要报道国产洛美沙星Ⅰ期临床试验研究结果。１２名健康志愿者分别口服４００ｍｇ单剂量及２００ｍｇ／次，每日两次，连服１４ｄ多剂量组均耐受良好，无明显不良反应。药代动力学结果表明，口服单剂量４００ｍｇ后，用微生物法测定血尿药浓度，所得主要药代动力学参数：Ｃ_ｍａｘ为３．７８±１．０８ｍｇ／ｌ；Ｔ_ｍａｘ为１．７１±１．０８ｈ；ＡＵＣ为２９．１６±７．８２ｍｇ·ｈ^－１Ｌ^－１；Ｔ_１／２为６．６８±０．８８ｈ；２４ｈ内原型药物在尿中排出量为７６．６±１８．２％，表明该药主要以原型从肾排泄。２００ｍｇ／次，每天２次给药组的稳态血药浓度约在０．５－２．２ｍｇ／ｌ或稍高水平。更多还原

【Abstract】 The results on the phase I clinical trial of lomefloxacin were reported.12 healthy volunteers were selected and divided randomly into 2 groups.They received a single dose of 400 mg or multiple doses of 200 mg twice daily for 14 days.respectively.The results showed that the drug was tolerated well.1 case of nausea was observed during this trial.But no significant change was found in any tested individuals, After an oral single dose of 400 mg, the concentrations were determined by a bioassay method,The mean pharmacokinetic parameters were as follows:C_max3.78±1.08 mg/l;T_max1.71±1.08 h;AUC 29.16±7.82 mg·h￣（-1）·L￣（-1）;T_1/26.68±0.88h.The parent drug excreted in the urine was 76.6% of the administrated dose within 24 hours. indicating that renal clearance represents the major route of elimination of this quinolone.In the multidose group.the plasma concentration of the drug varied from 0.5 to 2.2mg/l or higher.更多还原