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目的:对米格列奈片的人体药动学进行研究,为该药临床合理使用提供参考。方法:将20名健康志愿者随机平均分成2组(男女各半),一组为5 mg与15 mg 2个剂量单次口服给药,另一组为10 mg剂量单次口服给药与每天3次连续7 d的多次口服给药。采用HPLC-MS/MS法测定血药浓度,WinNonlin 6.3软件计算药动学参数,IBM SPSS Statistics 19软件对结果进行分析。结果:单剂量口服米格列奈片5 mg、10 mg、15 mg和多剂量口服10 mg后,血浆中米格列奈的AUC0→t分别为(846.2±149.6)、(1337.9±183.2)、(2785.3±261.3)、(1327.2±240.8)ng·h·mL-1,C max分别为(375.7±99.8)、(499.8±99.0)、(1189.4±133.9)、(781.7±319.7)ng·mL-1;T max分别为(0.9±0.4)、(1.0±0.5)、(1.1±0.5)、(0.9±0.4)h;t1/2分别为(1.1±0.2)、(1.3±0.2)、(1.4±0.3)、(1.2±0.3)h。结论:单剂量口服给药试验表明,在考察的剂量范围内,口服米格列奈在健康中国人体内的药动学过程呈现线性动力学特征;多剂量实验表明米格列奈在健康中国人体内几乎无蓄积现象;米格列奈在不同性别中国人群体内的药动学过程无明显差异。
Objective: To study the human pharmacokinetics of mitiglinide and provide a reference for the rational use of this medicine. Methods: Twenty healthy volunteers were randomly divided into two groups (male and female in half). One group was given a single oral dose of 5 mg and 15 mg and the other group was a single oral dose of 10 mg dose with daily 3 times for 7 consecutive days of oral administration. The plasma concentration was determined by HPLC-MS / MS, pharmacokinetic parameters were calculated by WinNonlin 6.3 software, and the results were analyzed by IBM SPSS Statistics 19 software. Results: AUC0 → t of mitiglinide in plasma after single oral administration of 5 mg, 10 mg and 15 mg of mitotaline and 10 mg of multidose orally were (846.2 ± 149.6) and (1337.9 ± 183.2), respectively (2785.3 ± 261.3) and (1327.2 ± 240.8) ng · h · mL-1, respectively, and the C max values were (375.7 ± 99.8), (499.8 ± 99.0), (1189.4 ± 133.9) and (781.7 ± 319.7) ng · mL- 1, Tmax were (0.9 ± 0.4), (1.0 ± 0.5), (1.1 ± 0.5), (0.9 ± 0.4) h respectively; t1 / 2 were (1.1 ± 0.2), (1.3 ± 0.2) ± 0.3), (1.2 ± 0.3) h. CONCLUSIONS: The single-dose oral administration test shows that the pharmacokinetics of oral mitiglinide in healthy Chinese people presents linear kinetics within the investigated dose range. Multiple dose experiments indicate that in healthy Chinese Almost no accumulation in vivo phenomenon; mitiglinide in different gender groups in China pharmacokinetic process no significant difference.