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建立测定人血浆中依普利酮浓度的HPLC-ESI-MS法。依普利酮血浆样品采用乙酸乙酯提取,色谱柱为反相色谱C18柱,流动相为10 mmol.L-1醋酸铵水溶液-甲醇(30∶70,v/v)。质谱离子源为电喷雾离子化(ESI)源,选择性离子检测方式检测;血浆样品在2～4000 ng.mL-1内线性良好,定量下限为2 ng.mL-1。本文采用该方法对健康受试者的人体药代动力学进行研究,3个单剂量(25 mg、50 mg和100 mg)口服给药后的药代动力学参数分别为t1/2:(4.9±2.1)、(4.7±1.5)、(5.9±1.2)h;AUC0-∞:(4402±1735)、(8150±2509)、(13783±4102)μg.h.L-1;MRT:(6.2±2.1)、(6.6±1.3)、(7.2±1.6)h;多剂量口服给药50 mg后药代动力学参数为t1/2:(6.1±1.7)h;AUCss:(10 071±4 220)μg.h.L-1;MRT:(8.1±2.3)h;DF:(3.2±1.0)。
A HPLC-ESI-MS method for the determination of eplerenone in human plasma was established. Eplerenone plasma samples were extracted with ethyl acetate. The column was reversed-phase C18 column and the mobile phase was 10 mmol·L-1 ammonium acetate-methanol (30:70, v / v). The mass spectrometry ion source was electrospray ionization (ESI) source and detected by selective ion detection method. The plasma sample showed a good linearity within 2 ~ 4000 ng.mL-1 with a lower limit of quantitation of 2 ng.mL-1. In this study, the pharmacokinetics of human subjects in healthy subjects were studied. The pharmacokinetic parameters of three single doses (25 mg, 50 mg, and 100 mg) after oral administration were t1 / 2: 4.9 ± 2.1), (4.7 ± 1.5), (5.9 ± 1.2) h; AUC0-∞: (4402 ± 1735), (8150 ± 2509), (13783 ± 4102) μg.hL- ), (6.6 ± 1.3), and (7.2 ± 1.6) h, respectively; the pharmacokinetic parameters of multiple doses of oral administration of 50 mg were t1 / 2: (6.1 ± 1.7) h; AUCss: .hL-1; MRT: (8.1 ± 2.3) h; DF: (3.2 ± 1.0).