国产氟罗沙星健康志愿者药物动力学研究

Pharmacokinetics study of fleroxacin in healthy volunteers

研究了７名健康志愿者口服单剂国产氟罗沙星４００ｍｇ后的药物动力学特征。用高效液相色谱法（ＨＰＬＣ）测定血清和尿中药物浓度。该药在体内转运过程以二室模型拟合为优，其显著特点是消除半衰期长（１１．２７ｈ）、血药峰浓度高（４．５９μｇ／ｍｌ）、表观分布容积大（０．８７Ｌ／ｋｇ）、血药时曲线下面积和系统清除率分别为６７．７８μｇｈ／ｍｌ和１０２．１ｍｌ／ｍｉｎ。尿药浓度在服药后２～４ｈ达到高峰为２９８±１１５μｇ／ｍｌ，４８～６０ｈ仍可达１４．３±８．４μｇ／ｍｌ。服药后２４、６０ｈ，尿药排泄率分别为５２．６％和６７．６％。

Fleroxacin is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of Gram negative and Gram positive bacteria. Seven healthy male volunteers received 400 mg of fleroxacin in tablet form orally. Drug concentrations were determined by a reversed phase high pressure liquid chromatogrphy (HPLC) method. Fleroxacin was characterized pharmacokinetically by a long elimination half life (11.27h) and high concentrations in plasma (4.59μg/ml). The volume of distribution clearly exceeded 0.6L/kg and suggested a good tissue penetrtion. The area under the plasma concentration time curve (AUC) amounted to 67.78μg/ml, and the total systemic clearance was 102.1ml/min. Within 60h, the cumulative urinary recovery of unchanged drug amounted to 67.6% of the given dose.