A fixed-dose combination of ticagrelor 90 mg and ASA 100 mg was bioequivalent to concomitant administration, with all 90% CIs for Cmax and AUC falling within the 80-125% range.
RCT (n=24)
Open-label
Randomized, two-period crossover
Does a fixed-dose combination of ticagrelor 90 mg and ASA 100 mg provide comparable bioavailability to concomitant administration of individual tablets in healthy volunteers?
A novel fixed-dose combination of ticagrelor 90 mg and ASA 100 mg is bioequivalent to the co-administration of individual tablets, providing a simplified option for dual antiplatelet therapy.
Effect estimate: Geometric mean ratio 100.3% (ticagrelor AUC0-48h) (95% CI 93.4-107.7)
Dual antiplatelet therapy (DAPT) with acetylsalicylic acid (hereafter referred to as ASA) and ticagrelor is the standard of care for secondary prevention for atherothrombotic events, particularly in patients with noncardioembolic cerebrovascular disease or coronary artery disease. However, prolonged DAPT requires multiple daily tablets, which can compromise adherence; a fixed-dose combination could reduce pill burden and improve treatment persistence. This study evaluated the comparative bioavailability of a fixed-dose combination (FDC) capsule of ticagrelor 90 mg/ASA 100 mg (test) versus the concomitant administration of ticagrelor 90 mg tablet plus ASA 100 mg tablet (reference) under fasting conditions in healthy Mexican volunteers. We applied a randomized, open-label, two-period crossover, single-dose design with a 7-day washout and quantified plasma concentrations by liquid chromatography-tandem mass spectrometry. Twenty-four subjects were enrolled. Geometric mean ratios (90% confidence intervals) for ticagrelor maximum plasma concentration and area under the plasma concentration-time curve from 0 to 48 h, were 111.5% (102.3-121.5), and 100.3% (93.4-107.7); for salicylic acid, 95.4% (90.1-100.9), and 101.5% (96.7-106.5). All 90% confidence intervals fell within the predefined 80-125% range, and both formulations were well tolerated. These findings support the FDC as an alternative that may simplify long-term DAPT for the secondary prevention of atherothrombotic events.
Tera‐Ponce等人（星期三）对健康志愿者（n=24）进行了随机对照试验。评估了泰卡格雷与阿司匹林（ASA）联合用药的固定剂量组合与90 mg泰卡格雷片加100 mg ASA片的同时给药的比较生物利用度（Cmax和AUC0-48h，分别用于泰卡格雷和水杨酸）（几何均值比100.3%（泰卡格雷 AUC0-48h），95% CI 93.4-107.7）。固定剂量的90 mg泰卡格雷和100 mg ASA组合与同时给药的生物等效，90%置信区间（CIs）对于Cmax和AUC均落在80-125%范围内。