Premium
Bioavailability of Triprolidine as a Single Agent or in Combination With Pseudoephedrine: A Randomized, Open‐Label Crossover Study in Healthy Volunteers
Author(s) -
Febbraro Salvatore,
Shea Tim,
Cravo Ana Santos
Publication year - 2020
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.777
Subject(s) - pseudoephedrine , medicine , crossover study , pharmacokinetics , bioavailability , bioequivalence , adverse effect , antihistamine , pharmacology , randomized controlled trial , anesthesia , ephedrine , alternative medicine , pathology , placebo
Abstract Antihistamines have been in clinical use for more than 70 years to treat allergic and nonallergic symptoms including relief from cold and flu symptoms. Despite their widespread use, pharmacokinetic (PK) data are sparse for older, first‐generation antihistamines. This phase 1 single‐center open‐label, randomized, single‐dose, 3‐way crossover trial evaluated the PK profiles of 2 doses of film‐coated triprolidine caplets (2.5 and 5 mg) compared with a reference combination tablet (triprolidine 2.5 mg + pseudoephedrine 60 mg) in 24 healthy adults. Blood samples were collected predose and at specified intervals across a 24‐hour period after administration, and triprolidine was quantified using liquid chromatography‐tandem mass spectrometry. Maximum plasma concentration of triprolidine for the 2.5 mg and dose‐normalized 5 mg single‐agent tablets were comparable (8.4 versus 7.1 ng/mL, respectively) and higher for the combination tablet (9.5 ng/mL). PK parameters, including time to maximum plasma concentration (∼1.5 hours) and elimination half‐life (∼4 hours), were comparable between the 3 treatment arms. The safety profile of this sedating antihistamine was as expected; however, adverse effects were reported in a markedly higher proportion of women than men. There were no significant sex differences in any of the measured PK parameters.