NCT02264041已完成1 期
The Effect of Cytochrome P 450 3A4 Inhibition by Itraconazole on the Single Oral Dose Pharmacokinetics of Cilobradine (an Open-label, Randomised, Single-dose, Two-way Crossover Study)
适应症
干预措施
相关药物
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 25
- 主要终点
- Maximum measured concentration of the analyte in plasma (Cmax)
研究概览
简要总结
Study to investigate the effect of cytochrome P 450 3A4 inhibition by itraconazole on the single dose pharmacokinetics of cilobradine
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 21 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy males according to the following criteria:
- •Based upon a complete medical history, including the physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests
- •1.1 No finding deviating from normal and of clinical relevance
- •1.2 No evidence of a clinically relevant concomitant disease
- •Age ≥21 and Age ≤55 years
- •BMI ≥18.5 and BMI < 30 kg/m2 (Body Mass Index)
- •Resting pulse rate (PR; after 10 min. in the supine position) of more than 55 bpm
- •Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation
排除标准
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological, ophthalmological, or hormonal disorders
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •History of relevant orthostatic hypotension, fainting spells or blackouts.
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
- •Intake of drugs with a long half-life (>24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
- •Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial.
- •Participation in another trial with an investigational drug within two months prior to administration or during the trial
- •Smoker (more than 10 cigarettes or 3 cigars or 3 pipes/day)
- •Inability to refrain from smoking on trial days
- •Alcohol abuse (more than 60 g/day)
- •Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
- •Excessive physical activities (within one week prior to administration or during the trial)
- •Any laboratory value outside the reference range that is of clinical relevance
研究组 & 干预措施
Cilobradine, high dose plus itraconazole
Experimental
main study
干预措施: Cilobradine, high dose (Drug)
Cilobradine, low dose plus itraconazole
Experimental
Pre-study
干预措施: Cilobradine, low dose (Drug)
Cilobradine, low dose plus itraconazole
Experimental
Pre-study
干预措施: Itraconazole (Drug)
Cilobradine, low dose
Active Comparator
Pre-study
干预措施: Cilobradine, low dose (Drug)
Cilobradine, high dose plus itraconazole
Experimental
main study
干预措施: Itraconazole (Drug)
Cilobradine, high dose
Active Comparator
main study
干预措施: Cilobradine, high dose (Drug)
结局指标
主要结局
Maximum measured concentration of the analyte in plasma (Cmax)
时间窗: up to 56 hours after administration of Cilobradine
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞)
时间窗: up to 56 hours after administration of Cilobradine
次要结局
- Time from dosing to Cmax (Tmax)(up to 56 hours after administration of Cilobradine)
- Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point (AUC0-tz)(up to 56 hours after administration of Cilobradine)
- Terminal rate constant in plasma (λz)(up to 56 hours after administration of Cilobradine)
- Number of subjects with clinically relevant findings in vital signs(up to 32 days)
- Occurrence of visual phenomena(up to 46 days)
- Number of subjects with clinically relevant findings in laboratory tests(up to 32 days)
- Number of subjects with clinically relevant findings in 12-lead electrocardiogram(up to 32 days)
- Assessment of tolerability by investigator on a 4-point scale(within 8 days after last PK sampling)
- Terminal half-life of the analyte in plasma (t1/2)(up to 56 hours after administration of Cilobradine)
- Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F)(up to 56 hours after administration of Cilobradine)
- Amount of parent compound excreted in urine with zero to 72 h in % of dose (fe0-tz)(up to 72 hours after administration of Cilobradine)
- Renal clearance of cilobradine (CLR,0-tz)(up to 72 hours after administration of Cilobradine)
- Mean residence time of the analyte in the body after p.o. administration (MRTpo)(up to 56 hours after administration of Cilobradine)
- Apparent clearance of the analyte in the plasma after extravascular administration (CL/F)(up to 56 hours after administration of Cilobradine)
- Number of subjects with adverse events(up to 46 days)
研究者
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