Relative Bioavailability Study of Riociguat Given Orally as a Crushed 2.5 mg Tablet Suspended in Applesauce, Crushed 2.5 mg Tablet Suspended in Water, and Whole 2.5 mg Tablet After a Continental Breakfast in Comparison to a Whole 2.5 mg Tablet Given in the Fasted State to Characterize the Pharmacokinetic Properties in Healthy Male Adult Subjects in a 4-fold Crossover Design
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Bayer
- 入组人数
- 48
- 主要终点
- Pharmacokinetics of riociguat in plasma by maximal concentration (Cmax)
研究概览
简要总结
To investigate relative bioavailability of crushed tablets suspended in apple sauce or water
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subject
- •Age: 18 to 45 years (inclusive) at the first screening examination
- •Ethnicity: white
- •Body mass index (BMI): >18 and <29.9 kg/m2
排除标准
- •Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination, or effects of the study drug will not be normal
- •History of coronary artery disease
- •Symptomatic postural hypotension (e.g. dizziness, lightheadedness)
- •History of bronchial asthma or any other airway disease
- •Smoking (former smokers who have stopped smoking at least 3 months before the first study drug administration may be included)
- •Clinically relevant findings in the ECG such as a second- or third-degree atrioventricular block, prolongation of the QRS complex over 120 ms or of the QTc interval (QT interval corrected for heart rate) over 450 ms
- •Systolic blood pressure below 100 or above 145 mmHg
- •Diastolic blood pressure below 50 or above 95 mmHg
- •Heart rate below 45 or above 95 beats per minute
研究组 & 干预措施
BAY63-2521 with Non sparkling water
Single dose of a whole 2.5 mg riociguat tablet (fasted) with 240 mL of non-sparkling water at room temperature
干预措施: Riociguat(Adempas,BAY63-2521) (Drug)
BAY63-2521 with applesauce
Single dose of a crushed 2.5 mg riociguat tablet suspended in 50 mL applesauce, to be eaten with a spoon (fasted)
干预措施: Riociguat(Adempas,BAY63-2521) (Drug)
BAY63-2521 with water
Single dose of a crushed 2.5 mg riociguat tablet suspended in a glass with 25 mL water, to be drunk and flushed twice with 25 mL water in the same glass (fasted)
干预措施: Riociguat(Adempas,BAY63-2521) (Drug)
BAY63-2521 after breakfast
Single dose of a whole 2.5 mg riociguat tablet taken within 5 minutes after the last bite of a continental breakfast (fed) with 240 mL of non-sparkling water at room temperature
干预措施: Riociguat(Adempas,BAY63-2521) (Drug)
结局指标
主要结局
Pharmacokinetics of riociguat in plasma by maximal concentration (Cmax)
时间窗: Multiple time ponits up to day 3
Pharmacokinetics of riociguat in plasma by Area under the plasma concentration time curve (AUC)
时间窗: Multiple time points up to day 3
次要结局
- Number of participants with adverse events as a measure of safety and tolerability(Up to 12 weeks)