Clinical Pharmacology Department, Hospital Universitario de La Princesa Instituto de Investigación Sanitaria La Princesa (IP), Universidad Autónoma de Madrid (UAM), C/ Diego de León, 62, 28006, Madrid, Spain.
Department of Research, Development and Innovation, FAES FARMA S. A., C. Vía de los Poblados 3, 28033, Madrid, Spain.
Drugs R D. 2024 Sep;24(3):405-414. doi: 10.1007/s40268-024-00480-8. Epub 2024 Aug 1.
Orodispersible tablets (ODT) rapidly dissolve in the oral cavity and can improve patient's convenience. This pharmacokinetic study assessed the bioequivalence of a novel 20 mg ODT formulation of bilastine compared with bilastine 20 mg tablets in healthy volunteers under fasting conditions.
A phase I, single-center, open-label, two-period, two-sequence crossover randomized clinical trial was conducted. The study comprised two periods, in which participants were administered a single oral dose of bilastine 20 mg in the form of ODT as the test product, or conventional tablets as the reference product, and a washout of 7 days between each period. Blood samples were collected for up to 72 h. Bioequivalence was established if the 90% confidence intervals of the C and AUC were within the acceptance range (80-125%). Safety was evaluated at the follow-up visit (days 4-7 after the second dose) and throughout the study.
A total of 42 healthy volunteers were randomized, and 41 completed the study. Pharmacokinetic parameters were comparable for both formulations after a single dose of 20 mg. Bilastine ODT and conventional tablets were bioequivalent as the 90% confidence intervals of the test over reference ratios were within the predefined range (80-125%). Both formulations were well tolerated and showed a similar safety profile.
Bilastine ODT was bioequivalent to the reference treatment formulated as conventional tablets when administered as a single oral dose of 20 mg under fasting conditions. Both formulations showed a similar tolerability and safety profile, with no serious adverse events or significant analytical alterations reported.
2019-004071-39. Date of authorization: 10 December 2019.
口崩片（ODT）在口腔中迅速溶解，可提高患者的便利性。这项药代动力学研究评估了新型 20 毫克比拉斯汀 ODT 制剂与空腹条件下健康志愿者中 20 毫克比拉斯汀片剂的生物等效性。
这是一项 I 期、单中心、开放标签、两周期、两序列交叉随机临床试验。该研究包括两个周期，每个周期中，参与者单次口服给予 20 毫克比拉斯汀的 ODT 制剂（试验产品）或常规片剂（参比产品），两次给药之间间隔 7 天。采集血样时间长达 72 小时。如果 C 和 AUC 的 90%置信区间在可接受范围内（80-125%），则认为具有生物等效性。在第二次给药后第 4-7 天（随访时）和整个研究过程中评估安全性。
共有 42 名健康志愿者被随机分组，41 名志愿者完成了研究。单次给予 20 毫克后，两种制剂的药代动力学参数相似。比拉斯汀 ODT 和常规片剂具有生物等效性，因为测试与参考的比值的 90%置信区间在预定范围内（80-125%）。两种制剂均耐受良好，具有相似的安全性特征。
在空腹条件下单次口服 20 毫克时，比拉斯汀 ODT 与常规片剂的参比治疗具有生物等效性。两种制剂的耐受性和安全性特征相似，未报告严重不良事件或明显的分析变化。
2019-004071-39。授权日期：2019 年 12 月 10 日。
