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Pharmacokinetic comparison between tablet of varenicline tartrate and orally disintegrating film of varenicline salicylate in healthy subjects
- Source :
- International journal of clinical pharmacology and therapeutics. 59(6)
- Publication Year :
- 2021
-
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 (Cmax) 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 (AUC0-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 Cmax and AUC0-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.
- Subjects :
- Drug
Male
media_common.quotation_subject
medicine.medical_treatment
Cmax
Administration, Oral
Pharmacology
Bioequivalence
Varenicline Tartrate
chemistry.chemical_compound
Pharmacokinetics
medicine
Humans
Pharmacology (medical)
Varenicline
media_common
Cross-Over Studies
business.industry
Crossover study
Healthy Volunteers
Salicylates
chemistry
Therapeutic Equivalency
Area Under Curve
Smoking cessation
business
Tablets
Subjects
Details
- ISSN :
- 09461965
- Volume :
- 59
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- International journal of clinical pharmacology and therapeutics
- Accession number :
- edsair.doi.dedup.....30fb8a4cf57063dda66e4898427cb7d8