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目的 :建立测定人血浆中西洛他唑含量的高效液相色谱 (HPLC)法 ,并研究西洛他唑片在健康人体内的药动学。方法 :色谱柱为HypersilC18柱(4 .6mm× 2 0 0mm ,5 μm) ,流动相为乙腈 水 (4 5∶5 5 ) ,流速 1.0ml·min-1,柱温 30℃ ,检测波长2 5 4nm ,西洛他唑血浆样品以 2mol·L-1NaOH 无水乙醚 (1∶4 )提取 ,以地西泮为内标。结果 :标准曲线线性范围 2 0～ 2 0 0 0 μg·L-1(r =0 .9999)。血浆中西洛他唑最低检测限为 10 μg·L-1。平均提取回收率为 80 .2 %± 3.6 % ,平均方法回收率为 97.0 %±3.8% ,日内RSD≤ 5 .8% ,日间RSD≤ 10 .1%。应用该法研究了 10例健康志愿者口服 10 0mg西洛他唑后的药动学 ;其体内过程符合二室模型 ,tmax为 3.5 8± 1.0 8h ,Cmax为 92 0± 2 30 μg·L-1,AUC0 -48为 11.0± 3.3mg·h-1·L-1。结论 :此法简便、快速 ,适用于药物分析 ,其药动学数据可为临床合理用药、新药研制及剂型改进提供理论依据
Objective: To establish a high performance liquid chromatography (HPLC) method for the determination of cilostazol in human plasma and to study the pharmacokinetics of cilostazol in healthy volunteers. METHODS: The column was Hypersil C18 (4.6 mm × 200 mm, 5 μm). The mobile phase consisted of acetonitrile and water (4 5:55). The flow rate was 1.0 ml · min-1. The column temperature was 30 ℃ and the detection wavelength was 25 4nm, cilostazol plasma samples with 2mol · L-1NaOH anhydrous ether (1: 4) to extract, with diazepam as internal standard. Results: The linear range of standard curve was 20 ~ 200 μg · L-1 (r = 0.9999). The lowest limit of detection of cilostazol in plasma was 10 μg · L-1. The average recovery was 80.2% ± 3.6%. The average recovery was 97.0% ± 3.8%. The intraday RSD was less than 5.8% and the intraday RSD was less than 10.1%. This method was used to study the pharmacokinetics of 10 cilostazol in 10 healthy volunteers. The in vivo process accorded with two-compartment model with tmax of 3.5 8 ± 1.08 h and Cmax of 92 0 ± 2 30 μg · L- 1, AUC0 -48 was 11.0 ± 3.3 mg · h-1 · L-1. Conclusion: This method is simple, rapid, suitable for drug analysis, and its pharmacokinetic data can provide theoretical basis for rational drug use, new drug development and dosage form improvement