Clinical Research Unit, Servicio de Farmacología Clínica, Clínica Universidad de Navarra, c/Pío XII, n° 36, 31008, Pamplona, Navarra, Spain.
Clin Drug Investig. 2013 May;33(5):375-81. doi: 10.1007/s40261-013-0076-y.
Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets and indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria. Several clinical trials have been performed in order to determine the efficacy and safety of bilastine. The aim of this trial was to study the absolute oral bioavailability of bilastine in humans.
Twelve male and female adults were recruited into a single centre for a randomized, single-dose, open-label, controlled two-arm crossover study with a minimum 14-day washout period between the two single doses. Two single doses of bilastine were administered: a 20-mg oral tablet and a 10-mg intravenous formulation. Blood and urine samples were collected between 0 and 72 h post each administration. The clinical trial was carried out under quality assurance and quality control systems with standard operating procedures to ensure that the study was conducted and data generated in compliance with the protocol, Good Clinical Practice standards, International Conference on Harmonisation and other applicable regulations.
Oral bioavailability of bilastine was 60.67 % with a 90 % parametric confidence interval of 53.79-67.56. The maximum bilastine concentration was measured 1.31 h after oral administration. Pharmacokinetic parameters were similar to those observed in previous studies. Tolerance to treatment was good, with no adverse events related to study medication.
The absorption of bilastine after oral administration to healthy subjects was rapid. The absolute oral bioavailability was moderate.
比拉斯汀（Bilaxten™）是一种新型的非镇静 H1 受体拮抗剂（抗组胺药），以口服片剂的形式开发，用于治疗过敏性鼻炎（季节性和常年性）和荨麻疹。已经进行了多项临床试验，以确定比拉斯汀的疗效和安全性。本试验旨在研究比拉斯汀在人体中的绝对口服生物利用度。
招募了 12 名男性和女性成年人进入一个中心，进行一项随机、单剂量、开放标签、对照的两臂交叉研究，两次单剂量之间有至少 14 天的洗脱期。给予两种单剂量的比拉斯汀：20mg 口服片剂和 10mg 静脉制剂。在每次给药后 0 至 72 小时内采集血样和尿样。临床试验在质量保证和质量控制系统下进行，采用标准操作程序，以确保研究按照方案、良好临床实践标准、国际协调会议和其他适用法规进行，并生成数据。
比拉斯汀的口服生物利用度为 60.67%，90%参数置信区间为 53.79-67.56。口服后最大比拉斯汀浓度在 1.31 小时测量到。药代动力学参数与之前的研究观察到的相似。治疗耐受性良好，无与研究药物相关的不良事件。
健康受试者口服比拉斯汀后吸收迅速。绝对口服生物利用度为中等。
