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首页> 外文期刊>International journal of clinical pharmacology and therapeutics >The pharmacokinetic and tolerability profile of varenicline in healthy Chinese volunteers.
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The pharmacokinetic and tolerability profile of varenicline in healthy Chinese volunteers.

机译：伐尼克兰在健康中国志愿者中的药代动力学和耐受性。

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Objective: Varenicline is a selective, nicotinic alpha4beta2 acetylcholine receptor partial agonist that has been licensed as a smoking cessation drug in more than 70 countries worldwide. The current study was conducted in order to evaluate its pharmacokinetic (PK) properties and tolerability in healthy volunteer Chinese smokers. Methods: This was an open-label, non-randomized study conducted over 17 days at a single center in China. Male and female subjects (18 - 45 years old) received a single, 1 mg dose of varenicline on days 1 and 10 as well as 1 mg varenicline twice daily (12-h dosing interval) on Days 4 - 9. Results: A total of 14 subjects (50% male) received varenicline as per study protocol for 8 days. The mean maximum plasma concentration of varenicline (Cmax) was 1.93-fold larger at steady state (reached on Day 8, after 4 days of repeat dosing) than following a single dose, showing accumulation of varenicline on repeat administration. Median values of tmax (time of occurrence of Cmax) were similar for both dosing regimens (3.0 and 2.5 h following single and multiple dosing, respectively). The mean elimination half-life following single and multiple dosing was 15.2 and 18.3 h, respectively. There was no evidence of time- or concentration-dependence in the PK of varenicline upon repeat dosing as the ratio of the area under the plasma concentration vs time curve (AUC) from time 0 - 12 h at steady state to the AUC from time 0 - 8 on Day 1 was nearly 1. The 2-sided 95% confidence intervals for this comparison included 1, demonstrating the linearity of the PK of varenicline for the single and multiple doses. Varenicline was safe and well-tolerated, adverse events were mild in severity and there were no abnormal laboratory tests. Conclusions: Varenicline 1 mg twice daily was safe and well-tolerated in a cohort of healthy male and female, 18- to 45-year-old Chinese smokers and demonstrated PK properties that were stable and reproducible and similar to those observed previously in Western subjects.
机译：目的：Varenicline是一种选择性的烟碱型α4beta2乙酰胆碱受体局部激动剂，已在全球70多个国家/地区获得许可，作为戒烟药物。进行本研究是为了评估其在健康的中国自愿吸烟者中的药代动力学（PK）特性和耐受性。方法：这是一项开放标签，非随机的研究，在中国的一个中心进行了17天。男性和女性受试者（18-45岁）在第1天和第10天接受一次1 mg的伐尼克兰剂量，在第4-9天每天两次（12小时给药间隔）接受1 mg伐尼克兰。 14名受试者（50％的男性）中有8天按照研究方案接受了伐尼克兰治疗。在稳定状态下（重复给药4天后第8天达到），伐尼克兰的平均最大血浆浓度（Cmax）比单一剂量大1.93倍，表明伐尼克兰在重复给药时蓄积。两种给药方案的tmax中值（Cmax的发生时间）均相似（单次和多次给药后分别为3.0小时和2.5小时）。单次和多次给药后的平均消除半衰期分别为15.2和18.3 h。没有证据表明重复给药后伐尼克兰的PK呈时间依赖性或浓度依赖性，因为稳态下从时间0到12 h的血浆浓度与时间曲线（AUC）到时间0到AUC的面积之比-第1天的8点接近1。此比较的2边95％置信区间包括1，这表明缬草酸单剂量和多次剂量PK呈线性。 Varenicline安全且耐受性良好，不良事件轻度且实验室检查未见异常。结论：在健康的男性和女性，18岁至45岁的中国吸烟者队列中，每天两次服用1毫克瓦伦尼克林是安全的，并且具有良好的耐受性，并且其PK特性稳定，可重现，并且与以前在西方受试者中观察到的相似。

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