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目的建立测定人血浆中屈昔多巴的方法,并应用于药代动力学研究。方法12例健康受试者单剂量口服屈昔多巴胶囊200 mg后,血样经高氯酸沉淀蛋白,通过HPLC-荧光检测法测定屈昔多巴的浓度,并运用3P87分析软件计算其药代动力学参数。结果屈昔多巴测定的线性范围为0.025~2μg/ml,其主要的药动学参数T1/2(108.50±30.78)min,曲线下峰面积(AUC)(185.74±26.41)μg.ml-1.min-1,消除率(CL)(1.08±0.08)ml/min,Tmax(99.90±10.05)min,Cmax(0.74±0.08)μg/ml,服药10 h后屈昔多巴几乎从血液中完全消除。结论本方法灵敏度高,重现性好,操作简便,可用于血浆样品中屈昔多巴的定性定量检测;屈昔多巴在体内的药代动力学过程符合二室模型。
Objective To establish a method for the determination of droxidopa in human plasma and its application in pharmacokinetic studies. Methods Twelve healthy subjects were dosed with 200 mg of droxidopa capsules. The blood samples were precipitated with perchloric acid and the concentrations of droxidopa were determined by HPLC-fluorescence. The pharmacokinetics were calculated using 3P87 software Kinetic parameters. Results The linear range of droxidopa was 0.025-2μg / ml. The main pharmacokinetic parameters were T1 / 2 (108.50 ± 30.78) min and peak area under the curve (AUC) (185.74 ± 26.41) μg.ml-1 (1.08 ± 0.08) ml / min, Tmax (99.90 ± 10.05) min and Cmax (0.74 ± 0.08) μg / ml respectively. After 10 hours of treatment, doxidopa almost completely disappeared from the blood eliminate. Conclusion The method has high sensitivity, good reproducibility and easy operation. It can be used for qualitative and quantitative detection of droxidopa in plasma samples. The pharmacokinetics of droxidopa in the body accords with the two-compartment model.