Park, Jin-Woo published the artcilePharmacokinetic comparisons of two different varenicline formulations in humans: Varenicline tartrate versus varenicline oxalate, COA of Formula: C17H19N3O6, the publication is International Journal of Clinical Pharmacology and Therapeutics (2020), 58(2), 121-127, database is CAplus and MEDLINE.
Varenicline is an effective drug for smoking cessation. The aim of the present study was to compare the pharmacokinetics and safety profies of two different varenicline formulations (varenicline tartrate (reference) and varenicline oxalate (test)), each containing 1 mg varenicline base in humans. A randomized, open-label, two-sequence, two-period, single-dose crossover study with a 2-wk washout period was conducted with 30 healthy male participants. Blood samples for the pharmacokinetic anal. of varenicline were collected up to 96 h following the administration of each drug. Pharmacokinetic parameters were also calculated, including the peak plasma concentration (Cmax), area under the plasma concentration-time curve (AUC) from time zero to the time of the last measurable concentration (AUClast) as well as AUC from time zero to infiity (AUCinf). ANOVA for pharmacokinetic equivalence was assessed using log-transformed Cmax and AUC values, and the geometric mean ratios (GMRs) and their 90% confience intervals (CIs) were assessed as well. The safety profies were also assessed. 27 participants completed the study. No signifiant differences were found for any pharmacokinetic parameters of varenicline between the two formulations. The observed average values of Cmax, AUClast, and AUCinf were 4.46 ng/mL, 97.68 ngxh/mL, and 101.60 ngxh/mL for reference and 4.54 ng/mL, 97.10 ngxh/mL, and 100.97 ngxh/mL for test, resp. The GMRs and 90% CIs for Cmax, AUClast, and AUCinf were 1.0106 (0.9626 – 1.0610), 0.9904 (0.9540 – 1.0282), and 0.9885 (0.9517 – 1.0268), resp. No clin. relevant changes were observed in the phys., biochem., hematol., electrocardiog., or urinalysis fidings during the study, and no serious adverse events were found. The results of the present study reveal that varenicline oxalate and varenicline tartrate have similar pharmacokinetic characteristics as varenicline, and that these two formulations exhibit pharmacokinetic equivalence to meet the regulatory criteria. Both varenicline formulations were generally well tolerated.
International Journal of Clinical Pharmacology and Therapeutics published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, COA of Formula: C17H19N3O6.
Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider