甲磺酸培氟沙星人体药代动力学研究

Study of Pefloxacin Mesylate Pharmacokinetics in Normal Volunteers after Single Oral Administration

目的 研究甲磺酸培氟沙星人体内药代动力学,为该药的临床评价提供依据.方法10名健康志愿者单剂量口服400mg甲磺酸培氟沙星后,采用HPLC法测定血药浓度,并拟合药代动力学参数.结果 8名受试者药时曲线为二室模型,2名为一室模型,平均达峰时间为1.19±0.48h,消除半衰期为11.61±2.53h,药时曲线下面积51.82±17.10μg·h·ml^(-1),吸收速率常数个体差异明显(1.69～923h^(-1)).结论 甲磷酸培氟沙星吸收迅速,半衰期长,体内分布广,有利于深部组织感染的治疗.

Aim Pefloxacin mesylate(PM ) was given orally in a single dose of 400mg to 10 healthy adultvolunteers to observe its pharmacokinetics. Methods The assay of plasma PM concentrationby HPLC method revealed that the concentration -time data in 8 subjects were fit for atwo - compartment model and in 2 subjects for a one - compartment model. Results The av-erage Tmax was 1. 19±0. 48h, elimination T1/2 11. 61± 2. 53 h and AUC 51. 82± 17. 10 μg·h·ml-1 . A considerable intersubject variability was noted in the constants of absorption rate. Pe-floxacin esylate was rapidly absorbed in gastrointestinal tract, and was widely distributed, whichindicated that it was of benefit to the therapy of deep tissue infections.