Bando T, Toyoshima H
Jpn J Antibiot. 1984 Jul;37(7):1279-88.
Serum and bile levels of fosfomycin sodium (FOM-Na) were evaluated and the pharmacokinetic parameters were estimated in 10 patients with various forms of biliary drainage (PTCD or T-tube). Clinical trials of FOM-Na were also performed in another 11 patients with bile duct infections and the clinical efficacy was estimated. Mean serum level of FOM-Na after drip infusion of 2 g fosfomycin sodium was 145.43 micrograms/ml at 1 hour, meanwhile bile level was 31.49 micrograms/ml at 2 hours. Serum level of FOM-Na was interpreted by the pharmacokinetic analysis after the damping GAUSS-NEWTON method using the one-compartment open model and bile level of FOM-Na by the damping GAUSS-NEWTON method and deconvolution method. Mean Vd was 12.16 L/body and half-time of serum level was 1.75 hours. Lag-time of bile level was 0.9 hour, Tmax 2.01 hours. The clinical efficacy of FOM-Na was determined excellent without any adverse effect. FOM-Na was remarkably effective in 91% of the patients. Hence, the first choice of FOM-Na against bile duct infections could be recommended.
对10例采用不同形式胆道引流（经皮肝穿刺胆道引流术或T管引流）的患者评估了磷霉素钠（FOM-Na）的血清和胆汁水平，并估算了药代动力学参数。另外还对11例胆管感染患者进行了FOM-Na的临床试验，并评估了临床疗效。静脉滴注2g磷霉素钠后1小时，FOM-Na的平均血清水平为145.43微克/毫升，同时2小时时胆汁水平为31.49微克/毫升。采用单室开放模型通过阻尼高斯-牛顿法对FOM-Na的血清水平进行药代动力学分析，采用阻尼高斯-牛顿法和反卷积法对FOM-Na的胆汁水平进行分析。平均分布容积为12.16升/体，血清水平半衰期为1.75小时。胆汁水平的滞后时间为0.9小时，达峰时间为2.01小时。FOM-Na的临床疗效判定为极佳，且无任何不良反应。91%的患者使用FOM-Na效果显著。因此，推荐FOM-Na作为治疗胆管感染的首选药物。
