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比较替利定和它的代谢物去甲替利定在不同性别中国健康志愿者中的药代动力学特征。9例(4例男性,5例女性)健康志愿者单次口服50 mg盐酸替利定口服液,在规定时间内采血,采用GC-NPD测定血药浓度,用非房室模型计算药代动力学参数。替利定和代谢物去甲替利定的主要动力学参数分别为:C_(max)(63.39±28.99)和(122.53±23.23)ng/mL;T_(max)(0.37±0.07)和(0.64±0.30)h;t_(1/2)(2.83±1.35)和(5.72±1.37)h;AUC_(0-∞)(101.59±41.85)和(577.13±189.77)ng·h/mL。替利定的男性和女性药动学参数分别为:C_(max)(73.88±40.88)和(55.01±15.16)ng/mL,T_(max)(0.37±0.08)和(0.36±0.08)h,t_(1/2)(4.05±1.07)和(1.86±0.41)h,AUC_(0-∞)(119.00±55.11)和(87.66±26.08)ng·h/mL。代谢物去甲替利定的男性和女性药动学参数分别为:C_(max)(108.82±27.88)和(133.49±12.56)ng/mL,T_(max)(0.94±0.13)和(0.40±0.09)h,t_(1/2)(4.66±1.18)和(6.57±0.84)h,AUC_(0-∞)(601.59±281.07)和(557.57±108.16)ng·h/mL。替利定的t_(1/2)男性比女性长,代谢物去甲替利定的T_(max)男性比女性慢,其它主要药代参数男性和女性之间没有统计学差异。受试者无严重不良事件发生,男性和女性的不良事件发生率有显著性差异。药代动力学研究显示,替利定口服液在应用于中国人时无需改变用药剂量,且性别因素影响不大。
Pharmacokinetic characteristics of tollitzin and its metabolite norfilizidine in healthy Chinese volunteers of different sexes were compared. 9 healthy volunteers (4 males and 5 females) received a single oral dose of 50 mg of tegliturone hydrochloride and blood samples were taken within the prescribed time. Plasma concentrations were determined by GC-NPD and non-compartmental model was used to calculate pharmacokinetics Learning parameters. The main kinetic parameters of telbivudine and metabolite norfilizidine were: C max (63.39 ± 28.99) and (122.53 ± 23.23) ng / mL, T max (0.37 ± 0.07) and (0.64 ± 0.30) h; t 1/2 (2.83 ± 1.35) and (5.72 ± 1.37) h; AUC 0-∞ (101.59 ± 41.85) and (577.13 ± 189.77) ng · h / mL, respectively. The pharmacokinetic parameters of tilidine were 73.88 ± 40.88 and 55.01 ± 15.16 ng / mL for C_ (max) (0.37 ± 0.08) and (0.36 ± 0.08) h, respectively, t 1/2 (4.05 ± 1.07) and (1.86 ± 0.41) h, AUC 0-∞ (119.00 ± 55.11) and (87.66 ± 26.08) ng · h / mL, respectively. The pharmacokinetic parameters of the metabolite norfilizidine male and female were as follows: C max (108.82 ± 27.88) and (133.49 ± 12.56) ng / mL, T max 0.94 ± 0.13 and 0.40 ± 0.09) h, t 1/2 (4.66 ± 1.18) and (6.57 ± 0.84) h, AUC 0 -∞ (601.59 ± 281.07) and (557.57 ± 108.16) ng · h / mL, respectively. There was no difference in t_ (1/2) male for telbivudine compared to female, and for metabolite desmethyltitidine, compared with female. The other major pharmacokinetic parameters were not statistically different between men and women. There were no serious adverse events in the subjects, and there was a significant difference in the incidence of adverse events between men and women. Pharmacokinetic studies have shown that, for oral administration in the application of Chinese do not need to change the dose, and sex has little effect.