NCT02171442已完成1 期
Metabolism and Pharmacokinetics of [14C]-BIBR 953 ZW After Administration of Single Doses of 5 mg [14C]-BIBR 953 ZW Intravenously or 200 mg [14C]-BIBR 1048 Oral Solution in a Group Comparison Design in 12 Healthy Male Volunteers.
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
- 10
- 主要终点
- [14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species
研究概览
简要总结
The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man.
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
- 30 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subjects as determined by results of screening
- •Signed written informed consent from each subject in accordance with the regulatory and legal requirements of the UK
- •Age between 30 and 55 years of age
- •Body Mass Index (BMI) of between 18.5 and 29.9 kg/m²
排除标准
- •Any of the findings from the medical examination (including BP, pulse rate and ECG) deviated from normal or were of clinical relevance
- •History of current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
- •History of relevant orthostatic hypotension, fainting spells and blackouts, or volunteers with diseases of the central nervous system (such as epilepsy) or psychiatric disorders
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the principal investigator
- •History of any bleeding disorder including prolonged or habitual bleeding
- •History of other hematologic disease
- •History of cerebral bleeding (e.g. after a car accident)
- •History of craniocerebral trauma
- •Intake of drugs with a long half life (≥ 24h) within 1 month prior to administration
- •Any drugs which may have had an influence on the results of the trial within 10 days prior to administration or during the trial
- •Any volunteers who had participated in another trial with an investigational drug within 3 months ( 4 months if the drug was a new chemical entity) prior to administration or during the trial
- •Exposition to radiation in the previous 12 months (i.e. serial x-rays, CT scan or barium meal)
- •Alcohol abuse (> 60 g/day)
- •Drug abuse
- •Blood donation within 12 weeks prior to administration or during the trial
- •Any excessive physical activities within 5 days prior to administration or during the trial
- •Any laboratory value outside the clinically accepted reference range
- •History of familial bleeding disorder
- •Platelets > 150 x 10-9 /l
- •Unable to defecate at least once a day every two days
研究组 & 干预措施
BIBR 953 ZW Intravenously
Experimental
干预措施: BIBR 953 ZW Intravenously (Drug)
BIBR 1048 Oral Solution
Active Comparator
干预措施: BIBR 1048 Oral Solution (Drug)
结局指标
主要结局
[14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species
时间窗: -12, 0 hours, 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 post dose
Total radioactivity in plasma and whole blood
时间窗: 168 hours
Total radioactivity in urine and faeces (excretion balance) over 168 h or until < 1% excreted in urine/faeces samples in a 24 h period
时间窗: over 168 hours or 24 hour period
Concentrations of BIBR 953 ZW in plasma over 168 h, estimation of the extent of gastrointestinal absorption
时间窗: 168 hours
Concentrations of BIBR 953 ZW in urine
时间窗: 168 hours
次要结局
- Cmax - Peak (maximum) plasma concentration of BIBR 953 ZW(Screening, day-1, day 1-day 8)
- tmax - time to reach the peak plasma concentration of BIBR 953 ZW(Screening, day-1, day 1-day 8)
- Ratio of radioactivity in blood cells and plasma (CE/CP)(0.5, 1, 2 ,4 ,8, 24 hours after oral study drug administration, 31min, 1, 2, 4, 8, 24h after start of infusion)
- Measurement of in vitro plasma protein binding of [14C]-BIBR 953 ZW(Screening, day-1, day 1-day 8)
- t1/2 - Terminal half-life derived from non-compartmental analysis of BIBR 953 ZW(Screening, day-1, day 1-day 8)
- AUC0-t - area under the plasma concentration vs. time curve from time zero to the time point for the last sample on the pharmacokinetic profile in which total radioactivity or active drug were reliably quantified) BIBR 953 ZW(Screening, day-1, day 1-day 8)
- AUC0-infinity - Area under the plasma concentration vs. time curve from time zero to infinity - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- MRT0-inf - the average amount of time a particle remains in a compartment or system, derived when the drug concentration profile is extrapolated to infinity) - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- MRT0-t - the average amount of time a particle remains in a compartment or system - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- CL renal - the apparent volume of the central compartment cleared of drug via renal excretion into the urine, per unit time - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- CLtot - the apparent volume of the central compartment cleared of drug per unit tim after intravenous dosing - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- CLtot/F - the apparent volume of the central compartment cleared of drug per unit time after extravascular dosing - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- Vss - apparent volume of distribution at steady state following intravenous administration - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- Vz/f - Volume of distribution during terminal phase after oral administration - BIBR 953 ZW(Screening, day-1, day 1-day 8)
- Cmax - Peak (maximum) plasma concentration for total radioactivity(up to day 8)
- tmax - time to reach the peak plasma concentration for total radioactivity(up to day 8)
- Occurence of Adverse events(Screening, upt to 10 days after study drug administration)
- Change from Baseline in physical examination(Screening, 8 to 10 days after study drug administration)
- Changes from Baseline in vital signs(Screening, 8 to 10 days after study drug administration)
- Change from Baseline in systolic and diastolic blood pressure(Screening, Day-1, day1, day2, day 8-10 after study drug administration)
- Change from Baseline in Pulse rate(Screening, Day-1, day1, day2, day 8-10 after study drug administration)
- Change from Baseline in 12-lead electrocardiogram (ECG)(Screening, Day-1, day1, day2, day 8-10 after study drug administration)
- Change from Baseline in clinical laboratory tests (hematology, clinical chemistry and urinanalysis)(Screening, day-1, day1, day2, day3, day 8-10 after study drug administration)
- Changes from baseline in activated partial thromboplastin time - aPTT(Screening, 1, 2, 24, 48 and 168 hours post dose administration)
- Changes from baseline in coagulation parameter INR - international normalized ratio prothrombin time(Screening, 1, 2, 24, 48 and 168 hours post dose administration)
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