人全血中环孢素A浓度的HPLC测定及药物动力学研究

Determination of cyclosporin A in whole blood by HPLC and its pharmacokinetic

建立了测定人全血中环孢素A的HPLC法。采用液-液萃取法处理血样,以环孢素D为内标,色谱柱DiamonsilC18柱,流动相为乙腈-甲醇-水(73∶5∶22),流速1.5ml/min,柱温60℃,检测波长210nm。环孢素A在50～1200ng/ml的浓度范围内线性关系良好,方法回收率为93.6%～108.0%,批内、批间RSD均小于10%。5名健康志愿者单剂量口服环孢素A500mg,Cmax、Tmax、T1/2b和AUC0～24分别为(2090.40±150.52)ng/ml、(1.30±0.27)h、(6.84±0.61)h和(9977.19±1260.63)h·ng·ml-1。

A HPLC method for determination of cyclosporin A in whole blood was established. The drug wasextracted from whole blood by the liquid-liquid extraction, using cyclosporin D as the internal standard. A C18 column wasused with the mobile phase of methanol-acetonitrile-water (73∶5∶22) at the detection wavelength of 210nm. The flowrate was 1.5ml/min. The column temperature was 60℃. The calibration curve was linear in the concentration range of 50～1200ng/ml. The recoveries were 93.6%～108.0%. The RSDs of intra- and inter-batch were less than 10%. A single dose of500mg cyclosporin A solution was given to 5 volunteers. The pharmacokinetics parameters: Cmax, Tmax, T1/2b and AUC0~24 were(2090.40±150.52)ng/ml, (1.30±0.27)h, (6.84±0.61)h and (9977.19±1260.63)h·ng·ml-1, respectively.