Int J Clin Pharmacol Ther. 2021 Jun;59(6):478-484. doi: 10.5414/CP203953.
Varenicline is an efficacious aid for smoking cessation. In this study, the pharmacokinetics and safety were compared between film-coated tablets of varenicline tartrate (reference drug) and the newly developed orally disintegrating films of varenicline salicylate (test drug), both of them contained 1 mg of varenicline.
A randomized, open-label, single-dose, two-sequence, two-period crossover study was conducted in healthy male subjects. Serial blood samples were obtained for up to 72 hours in each period, with a washout period of 7 days or more. The pharmacokinetic parameters were calculated using the noncompartmental method. Safety profiles were assessed throughout the study.
A total of 28 subjects completed the study. The plasma varenicline concentration-time profiles were similar for the two study drugs. The maximum plasma varenicline concentration (C) was 5,768.95 ng/L (mean) and 5,780.55 ng/L for the test drug and reference drug, respectively. The areas under the concentration-time curve from time 0 to the last measurable time point (AUC) were 94,086.30 h×ng/L and 89,958.55 h×ng/L for the test drug and reference drug, respectively. The geometric mean ratios (90% confidence intervals) of the test drug to the reference drug for C and AUC were 0.9955 (0.9488 - 1.0444) and 1.0449 (0.9848 - 1.1088), respectively, which fell within the bioequivalence range of 0.8 - 1.25. There was no difference in safety between the study drugs.
The pharmacokinetics and safety profiles were similar between the two study drugs. The orally disintegrating film of varenicline salicylate can be an alternative to varenicline tartrate tablets.
伐伦克林是一种有效的戒烟辅助药物。在这项研究中，比较了酒石酸伐伦克林（参比药物）和新开发的水杨酸伐伦克林口崩片（试验药物）的药代动力学和安全性，两者均含有 1 毫克伐伦克林。
这是一项在健康男性受试者中进行的随机、开放标签、单剂量、两序列、两周期交叉研究。每个周期最多采集 72 小时的连续血样，洗脱期为 7 天或更长时间。采用非房室法计算药代动力学参数。整个研究过程中评估安全性概况。
共有 28 名受试者完成了研究。两种研究药物的伐伦克林血浆浓度-时间曲线相似。最大血浆伐伦克林浓度（C）分别为 5768.95 纳克/升（平均值）和 5780.55 纳克/升，试验药物和参比药物。从 0 时间到最后可测量时间点的浓度-时间曲线下面积（AUC）分别为 94086.30 小时×纳克/升和 89958.55 小时×纳克/升，试验药物和参比药物。C 和 AUC 的试验药物与参比药物的几何均数比值（90%置信区间）分别为 0.9955（0.9488-1.0444）和 1.0449（0.9848-1.1088），均在 0.8-1.25 的生物等效范围内。两种研究药物的安全性无差异。
两种研究药物的药代动力学和安全性特征相似。水杨酸伐伦克林口崩片可以替代酒石酸伐伦克林片。
