Grim Jiri, Armogida Marianna, Kachroo Preeti, Siddiqui Kamran, Cavinato Mauro, Araga Mako
Quinta-Analytica, Praha, Czech Republic.
Haleon CH SARL, Nyon, Switzerland.
Curr Ther Res Clin Exp. 2024 Feb 1;100:100734. doi: 10.1016/j.curtheres.2024.100734. eCollection 2024.
A new oral paracetamol formulation with the same paracetamol quantity (24 mg/mL) as a marketed formulation but with finer active ingredient particle size and lower amounts of maltitol (5.85 g/dose in the test formulation vs 7.25 g/dose in the reference formulation) and sorbitol (2.4 g/dose vs 2.83 g/dose) was developed.
Establish the bioequivalence of the new pediatric formulation (test treatment) compared with the marketed formulation (reference treatment).
This Phase I, open-label trial assigned healthy adult volunteers to a single 42-mL (1 g para-cetamol) dose of test or reference treatment. Participants received both treatments in a randomized order separated by a 72-hour washout period. The primary endpoints were AUC (AUC vs time curve from time 0 to last measurable sampling timepoint), C, and t. Safety assessments included adverse event, clinical laboratory, and physical examination data.
Thirty-five participants were randomized and treated. The study population was 42.9% women (57.1% men) with a median age of 30 years; most participants were non-Hispanic White. Mean C values were comparable between test and reference products, with a median t of 1.00 hour for both. The test/reference ratios (%) (90% CI) for AUC and C were 98.69% (96.46, 100.97) and 100.73% (95.63, 106.10), respectively. There were no adverse events or deaths.
The new paracetamol formulation is bioequivalent to the marketed formulation.
研发了一种新的口服对乙酰氨基酚制剂，其对乙酰氨基酚含量（24毫克/毫升）与市售制剂相同，但活性成分粒径更细，麦芽糖醇含量更低（试验制剂为5.85克/剂量，参比制剂为7.25克/剂量），山梨醇含量也更低（分别为2.4克/剂量和2.83克/剂量）。
确定新的儿科制剂（试验治疗）与市售制剂（参比治疗）的生物等效性。
这项I期开放标签试验将健康成年志愿者随机分配至单剂量42毫升（1克对乙酰氨基酚）的试验或参比治疗。参与者以随机顺序接受两种治疗，间隔72小时的洗脱期。主要终点为AUC（从时间0至最后可测量采样时间点的AUC与时间曲线）、Cmax和tmax。安全性评估包括不良事件、临床实验室和体格检查数据。
35名参与者被随机分组并接受治疗。研究人群中女性占42.9%（男性占57.1%），中位年龄为30岁；大多数参与者为非西班牙裔白人。试验产品和参比产品的平均Cmax值相当，两者的中位tmax均为1.00小时。AUC和Cmax的试验/参比比值（%）（90%CI）分别为98.69%（96.46，100.97）和100.73%（95.63，106.10）。未发生不良事件或死亡。
新的对乙酰氨基酚制剂与市售制剂生物等效。
