目的 研究中国健康志愿者单剂量口服2.0、4.0 g依卡倍特二钠颗粒后的药代动力学行为,并评价药代动力学参数在2.0~4.0 g范围内剂量相关性.方法 10名健康志愿者,随机交叉试验,分别单剂量口服依卡倍特二钠颗粒2.0、4.0 g;测定给药后36 h内的血药浓度.结果 单剂量口服2.0、4.0 g依卡倍特二钠颗粒后,依卡倍特的t1/2分别为(11±5)h和(9±4)h,达峰浓度(Cmax)分别为(4 998±982)ng/mL和(11 699±4 143)ng/mL,AUC0～t分别为(43 863±10 341)ng·h-1·mL-1和(92 492±30 915)ng·h-1·mL-1,AUC0～∞分别为(48 611±15 029)ng·h-1·mL-1和(99 628±35 993)ng·h-1·mL-1.结论 在2.0~4.0 g剂量范围内依卡倍特呈线性药代动力学,Cmax、AUC的升高与剂量成正比.%Objective The purposes of the study were to characterize the pharmacokinetics of ccabct disodium single oral administrations of 2. 0, 4. 0 g in healthy subjects, and to assess the dose proportionality of ccabct over the dose range (2. 0~4. 0 g). Methods In a randomized crossover study, ten healthy subjects took single oral administrations of 2. 0, 4. 0 g ccabct disodium. Plasma concentrations were determined at selected time intervals for 36 hours. Results The elimination half-life of ccabct disodium after po 2. 0, 4. 0 g ccabct disodium were (11 ± 5) h and (9 ± 4) h, respectively. The peak plasma concentration (Cmax) were (4 998 ± 982) ng/mL and (11 699 ± 4 143) ng/mL, AUQ0~t were (43 863 ± 10 341 ) ng·h-1·mL-1 and (92 492 ± 30 91 ) ng·h-1·mL-1, AUC0~∞ were (48 611 ± 15 029)ng·h-1·mL-1 and (99 628 ± 35 993)ng·h-1·mL-1 , respectively. Conclusion Ecabet disodium exhibits a linear pharmacokinctic profile at the doses in the range of 2. 0~4. 0 g. Dosc-dcpcnd-cnt paramctcrs(Cmax , AUC)incrcascd in an approximately dose-proportional manner from 2. 0 g to 4. 0 g.
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