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目的 :测定司帕沙星在感染患者体内的药物代谢动力学。方法 :HPLC法测定 10例患者单剂量口服司帕沙星 2 0 0mg后血清和尿中药物浓度并计算药代动力学参数。结果 :司帕沙星血清药物浓度 -时间曲线符合一级吸收开放二室模型。药物吸收有一较长延滞期 ,平均为 (0 .2 5± 0 .12 )h ,吸收相T1/ 2 平均 (0 .88± 0 .17)h ,消除相T1/ 2 平均 (13.2 2± 2 .78)h,达峰时间(3.99± 0 .40 )h ,曲线下面积 (13.5 6± 3.98)mg·h·L-1,尿药消除率 (0 .75± 0 .40 )L·h-1,尿中原型药物 2 4h排出率为 8%~ 13% ,平均为 (10 .16± 1.46 ) % ,并且集中在 8h以后排出。结论 :司帕沙星片具有长效作用。
OBJECTIVE: To determine the pharmacokinetics of sparfloxacin in infected patients. Methods: The serum and urinary concentrations of sparfloxacin 200 mg in 10 patients were determined by HPLC. The pharmacokinetic parameters were calculated. Results: Sparfloxacin serum drug concentration-time curve in line with the first-order absorption and opening two-compartment model. The drug absorption had a longer lag phase, with an average of (0.25 ± 0.12) h, an average T1 / 2 absorption phase (0.88 ± 0.17) h, and an average phase elimination T1 / 2 of 13.2 ± 2 (P <0.01) .78) h, peak time (3.99 ± 0.40) h, area under the curve (13.56 ± 3.98) mg · h · L -1, urinary drug elimination rate (0.75 ± 0.40) L · h -1, urinary prototyping drugs 2 4h 8% ~ 13%, an average of (10.16 ± 1.46)%, and concentrated in 8h after discharge. Conclusion: Sparfloxacin tablets have a long-term effect.