Metabolism and Pharmacokinetics of [14C]-DK-AH 269 CL After Administration of Single Doses of 5 mg [14C]-DK-AH 269 CL Intravenously and 10 mg [14C]-DK-AH 269 CL as Oral Solution in a Parallel-group Design in 12 Healthy Male Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 12
- 主要终点
- Maximum measured concentration of the analytes in plasma (Cmax)
研究概览
简要总结
- To investigate absorption, metabolism and excretion of [14C]-DK-AH 269 CL after oral and intravenous administration in healthy volunteers
- To assess the safety and tolerability of DK-AH 269 CL after oral and intravenous administration to healthy volunteers
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 50 Years 至 65 Years（Adult, Older Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •50 to 65 years of age
- •Body Mass Index (BMI) of 19.9 to 29.9 kg/m2
- •Resting heart rate (HR) (after 5 min. in the supine position) of more than 55 bpm
- •All volunteers will have given their written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation.
排除标准
- •Any finding at the medical examination (including BP, HR and ECG) deviating from normal and of clinical relevance
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, hematological/oncological, immunological or hormonal disorders
- •Diseases of the central nervous system 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 ten half-lives of the respective drug before enrolment in the study
- •Use of any drugs which might influence the results of the trial within two weeks prior to administration or during the trial
- •Participation in another trial with an investigational drug (≤ two months prior to administration or during the trial)
- •Smoker (> 10 cigarettes or > 3 cigars of > 3 pipes/day)
- •Inability to refrain from smoking on trial days
- •Alcohol abuse (> 60 g/day)
- •Drug abuse
- •Blood donation (≥ 100 mL within 2 months prior to administration or during the trial)
- •Excessive physical activities (within the last week before the study)
- •Any laboratory value outside the reference range and of clinical relevance
- •Inability to comply with dietary regimen of study centre
- •Not necessarily clinically relevant abnormalities, but specific exclusion criteria for the drugs under study or for the study:
- •Subjects at increased risk for development of cardiac arrhythmia (e.g. family history of long QT syndrome or sudden cardiac death)
- •ECG: PR interval > 210 ms
- •HR at rest ≤ 55 beats per minute (bpm)
- •Relevant ophthalmological disease
研究组 & 干预措施
[14C]-DK-AH 269 CL intravenous
干预措施: [14C]-DK-AH 269 CL, solution for infusion (Drug)
[14C]-DK-AH 269 CL oral
干预措施: [14C]-DK-AH 269 CL, drinking solution (Drug)
结局指标
主要结局
Maximum measured concentration of the analytes in plasma (Cmax)
时间窗: Up to 96 hours after start of treatment
Area under the concentration-time curve of the analytes in plasma (AUC)
时间窗: Up to 96 hours after start of treatment
Time from dosing to the maximum concentration of the analytes in plasma (tmax)
时间窗: Up to 96 hours after start of treatment
Terminal rate constant of the analytes in plasma (λz)
时间窗: Up to 96 hours after start of treatment
Terminal half-life of the analytes in plasma (t1/2)
时间窗: Up to 96 hours after start of treatment
Mean residence time of the analytes in the body after intravenous administration (MRT)
时间窗: Up to 96 hours after start of treatment
Mean residence time of the analytes in the body after oral administration (MRTpo)
时间窗: Up to 96 hours after start of treatment
Apparent clearance of the analytes in plasma following extravascular administration (CL/F)
时间窗: Up to 96 hours after start of treatment
Total clearance of the analytes in plasma following intravascular administration (CL)
时间窗: Up to 96 hours after start of treatment
Apparent volume of distribution of the analytes during the terminal phase λz following extravascular administration (Vz/F)
时间窗: Up to 96 hours after start of treatment
Volume of distribution at steady state (Vss)
时间窗: Up to 96 hours after start of treatment
Fraction of analytes eliminated in urine from 0 to the time of the last quantifiable data point (fe0-tz)
时间窗: Up to 120 hours after start of treatment
Fraction of analytes eliminated in faeces from 0 to the time of the last quantifiable data point (fefaeces,0-tz)
时间窗: Up to 120 hours after start of treatment
Renal clearance of the analytes from 0 to the time of the last quantifiable data point (CLR,0-tz)
时间窗: Up to 120 hours after start of treatment
Fraction of dose absorbed, based on radioactivity data (Fa)
时间窗: Up to 96 hours after start of treatment
Absolute bioavailability of the analytes after oral administration (F)
时间窗: Up to 96 hours after start of treatment
Ratio of CBlood cells/Cplasma [14C]-radioactivity
时间窗: Up to 96 hours after start of treatment
Number of patients with clinically significant findings in vital signs
时间窗: up to 12 days after last drug administration
blood pressure, heart rate
Number of patients with clinically significant findings in 12-lead ECG
时间窗: up to 12 days after last drug administration
Number of patients with clinically significant findings in 2-lead ECG (telemetry)
时间窗: up to 90 minutes after start of treatment
Clinically significant changes from baseline in physical examination
时间窗: Pre-dose, and 12 days after last drug administration
Occurrence of visual phenomena
时间窗: up to 120 hours after start of treatment
questionnaire
Number of patients with clinically significant findings in clinical laboratory tests
时间窗: up to 12 days after last drug administration
次要结局
未报告次要终点