Abstract

Objective: 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.
Materials and methods: 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.
Results: 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_max) 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_0–t) 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_max and AUC_0–t 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.
Conclusion: 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.

Author Details

Authors

• Eunwoo Kim¹
• Jun Gi Hwang^{1, 2}
• Su Jun Park³
• Ji Young Han³
• Young-Sim Choi²
• Se-Rin Park²
• Kyung-Sang Yu¹
• Min Kyu Park²
• SeungHwan Lee^{1, 4}

Departments

• ¹ Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul,
• ² Department of Clinical Pharmacology and Therapeutics, Chungbuk National University Hospital, Cheongju-si, Chungcheongbuk-do,
• ³ CTCBIO Inc., Ansan-si, Gyeonggi-do, and
• ⁴ Clinical Trials Center, Seoul National University Hospital, Seoul, Republic of Korea

Address

SeungHwan Lee, 
MD, PhD
Department of Clinical Pharmacology and Therapeutics
Seoul National University College of Medicine and Hospital
101 Daehak-ro, Jongno-gu,
Seoul 03080, 
Republic of Korea
Email: [email protected]

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