2023 年第 9 期 第 18 卷

高原世居藏族健康人中苯磺酸氨氯地平的药代动力学特征研究

Study on pharmacokinetic characteristics of amlodipine besylate among Tibetan healthy human body living in plateau

作者：张瑞格桑罗布黄菊次白索娜央宗次仁卓玛

英文作者：Zhang Rui Gesangluobu Huang Ju Cibai Suonayangzong Cirenzhuoma

单位：西藏自治区人民医院西藏高原医学研究所西藏自治区人类适应高原转化医学研究重点实验室，拉萨850000

英文单位：People′s Hospital of Tibet Autonomous Region Institute of Tibet Plateau Medical Research Key Laboratory of Translational Medical Research for Human Adaptation to Plateau in Tibet Autonomous Region Lhasa 850000 China

关键词：苯磺酸氨氯地平；药代动力学；高原世居藏族健康人体

英文关键词：Amlodipinebesylate;Pharmacokinetics;Tibetanhealthyhumanbodylivinginplateau

• 摘要：

• 目的  探究高原世居藏族健康人中苯磺酸氨氯地平的药代动力学特征。方法 招募8名高原世居藏族健康受试者，给予口服单剂量苯磺酸氨氯地平5 mg，给药前0 h和给药后1、2、4、8、24、48、72 h采集外周静脉血，采用高效液相色谱-质谱/质谱联用法测定血浆苯磺酸氨氯地平浓度，采用Drug And Statistics 3.0软件计算药代动力学参数。结果 8名藏族健康受试者单次口服5 mg苯磺酸氨氯地平的平均药代动力学参数如下：达峰时间为(4.4±2.5)h，最大血药浓度为（3.1±0.5）μg/L，半衰期为（40±13）h，0～72 h和0～∞ h时的血浆药物浓度-时间曲线下面积分别为（115±11）μg·h/L和（159±16）μg·h/L。结论 苯磺酸氨氯地平在高原地区的平均达峰时间可能与高原环境对消化系统的影响有关，高原环境造成胃肠黏膜屏障的改变、损伤等可能加快了药物的吸收，导致达峰时间缩短。

• Objective To investigate the pharmacokinetic characteristics of amlodipine besylate among Tibetan healthy human body living in plateau. Methods A total of 8 Tibetan healthy subjects living in plateau were recruited for this study，and all subjects were given a single dose of 5 mg of amlodipine besylate orally, and venous blood samples were taken at time points of 0 h before administration and 1, 2, 4, 8, 24, 48, 72 h after administration. High performance liquid chromatography-mass spectrometry/mass spectrometry was used to determine amlodipine besylate concentration in plasma, and Drug And Statistics 3.0 software was used to calculate the pharmacokinetic parameters. Results The average pharmacokinetic parameters of 8 Tibetan healthy subjects who were given a single dose of 5 mg of amlodipine besylate orally were as follows, the peak time was (4.4±2.5)h, the maximum plasma drug concentration was (3.1±0.5)μg/L, the half-life period was (40±13)h, the areas under curve of the plasma drug concentration-time at 0-72 h and 0-∞ h were (115±11)μg·h/L and (159±16)μg·h/L respectively. Conclusions  sThe average peak time of amlodipine besylate in plateau areas may be related to the impact of plateau environment on the digestive system. Changes and damages to the gastrointestinal mucosal barrier caused by plateau environment may accelerate the absorption of the drug, resulting in a shorter peak time.