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目的 :建立反相高效液相色谱法测定血浆中依帕司他浓度 ,研究该药物在人体内的药代动力学。方法 :血浆样品用甲醇沉淀蛋白后直接进样 ,选地西泮作内标。采用 μBondapakC18(30 0mm× 3.9mm ,1 0 μm)柱 ,流动相 :甲醇 0 .0 1mol·L-1K3 PO4 乙腈 (5 0∶37∶1 3) ,流速 1 .4ml·min-1,设程序波长 0～ 4min 389nm ,4～ 7min 2 37nmUV检测。结果 :该方法回收率为1 0 1 .0 9%～ 1 0 5 .97% ,最低检测浓度为 5 .1ng·ml-1,日内RSD <4.48% (n =5 ) ,日间RSD <4.5 3% (n =5 ) ,线性范围 :2 0 .4～ 1 2 75 0ng·ml-1。 1 0例健康青年志愿者单剂量 po依帕司他片剂 5 0mg后 ,达峰时tmax为 (1 .79± 0 .5 7)h ,峰血药浓度cmax为(3840 .6± 96 8.5 )ng·ml-1,消除半衰期t1/2 β为 (1 .1 1± 0 .35 )h。结论 :本法快速 ,准确 ,灵敏 ,能较好地满足依帕司他临床药代动力学研究需要。
Objective: To establish a method for the determination of epalrestat in plasma by reversed-phase high performance liquid chromatography (RP-HPLC) and to study its pharmacokinetics in human. Methods: Plasma samples were precipitated with methanol directly into the sample, select diazepam as internal standard. The mobile phase was methanol 0. 01mol·L-1K3 PO4 acetonitrile (50:37:1), the flow rate was 1.4ml · min-1 using μ Bondapak C18 (300 mm × 3.9 mm, 10 μm) Wavelength 0 ~ 4min 389nm, 4 ~ 7min 2 37nmUV detection. Results: The recoveries of this method ranged from 101.0% to 105.997% with a minimum detectable concentration of 5. 1 ng · ml-1, an intraday RSD of 4.48% (n = 5) and a daytime RSD of 4.5 3% (n = 5), linear range: 20.4 ~ 1 2 75 0 ng · ml-1. The peak value of tmax was (1.79 ± 0.57) h and the peak plasma concentration cmax was (3840 ± 6 ± 8.5) 8.5 after single dose po povastatin tablets ) ng · ml-1, the elimination half-life t1 / 2 β was (1.1 ± 0.35) h. Conclusion: The method is rapid, accurate and sensitive and can meet the needs of clinical pharmacokinetics of epalrestat.