NCT02170584已完成1 期
Tolerability of Single Rising Doses of 0.1 mg, 1 mg, and 5 mg BIBR 953 ZW IV (Placebo-controlled in Each Dose Group; Substudy 1) and Absolute and Relative Bioavailability of 100mg BIBR 1048 Tablet and of Solution and of 1 mg or 5 mg BIBR 953 ZW IV (Randomized, Three-way Crossover; Substudy 2).
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
- 30
- 主要终点
- AUC0-inf (Area under the plasma concentration-time curve extrapolated to infinity)
研究概览
简要总结
Two substudies to assess (1) the tolerability of BIBR 953 ZW intravenous infusion at 0.1, 1 and 5 mg BIBR 953 ZW and (2) the absolute bioavailability of 100mg BIBR 1048 administered as 'acid free' tablet formulation (TF1) and (3) the bioavailability of the 100 mg tablet of BIBR 1048 relative to the tartaric acid solution of 100 mg dose strength and (4) the absolute bioavailability of the 100 mg tartaric acid solution of BIBR 1048 MS.
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
- Double
入排标准
- 年龄范围
- 18 Years 至 50 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 in accordance with GCP and local legislation
- •Age ≥ 18 and ≤ 50 years
- •Broca ≥ - 20% and ≤ + 20%
排除标准
- •Any findings of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
- •History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
- •History of orthostatic hypotension, fainting spells and blackouts
- •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 investigator
- •any bleeding disorder including prolonged or habitual bleeding
- •other hematologic disease
- •cerebral bleeding (e.g. after a car accident)
- •commotio cerebri
- •Intake of drugs with a long half-life (>24 hours) within 1 month prior to administration
- •Use of any drugs which might influence the results of the trial within 10 days prior to administration or during trial
- •Participation in another trial with an investigational drug within 2 months prior to administration or during trial
- •Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
- •Alcohol abuse (> 60 g/day)
- •Drug abuse
- •Blood donation within 1 month prior to administration or during the trial
- •Excessive physical activities within 5 days prior to administration or during the trial
- •Any laboratory value outside the clinically accepted reference range
- •History of any familial bleeding disorder
- •Thrombocytes < 150000/µl
研究组 & 干预措施
BIBR 953 ZW IV
Experimental
干预措施: BIBR 953 ZW IV (Drug)
BIBR 1048 MS oral solution
Active Comparator
干预措施: BIBR 1048 MS oral solution (Drug)
BIBR 1048 MS tablet
Experimental
干预措施: BIBR 1048 MS tablet (Drug)
BIBR 953 ZW IV Placebo
Placebo Comparator
干预措施: BIBR 953 ZW IV Placebo (Drug)
结局指标
主要结局
AUC0-inf (Area under the plasma concentration-time curve extrapolated to infinity)
时间窗: up to 48 hours after drug administration
AUC0-tf (Area under the plasma concentration-time curve up to the last quantifiable plasma concentration)
时间窗: up to 48 hours after drug administration
Cmax (Maximum plasma concentration after oral administration)
时间窗: up to 48 hours after drug administration
Cumulative urinary excretion of BIBR 953 ZW administered intravenously
时间窗: up to 48 hours after drug administration
次要结局
- changes in activated partial thromboplastin time (aPTT )(up to 48 hours after drug administration)
- changes in prothrombin time (PT)(up to 48 hours after drug administration)
- C29 (Plasma concentration of BIBR 953 ZW at 29 minutes after the start of the 30 min. infusion)(29 minutes after start of infusion)
- t1/2 (terminal half-life)(up to 48 hours after infusion)
- CLtot (total clearance of drug from plasma)(up to 48 hours after infusion)
- CLren (renal clearance from plasma)(up to 48 hours after infusion)
- MRTdisp (Mean time of residence of drug molecules in the body after intravascular administration)(up to 48 hours after infusion)
- Vss (apparent volume of distribution at steady state)(up to 48 hours after infusion)
- Vz (Apparent volume of distribution during the terminal elimination phase)(up to 48 hours after infusion)
- MRTtot (total mean residence time)(up to 48 hours after oral administration)
- CLtot/F (total clearance after oral administration)(up to 48 hours after oral administration)
- tmax (time to reach the peak plasma concentration)(up to 48 hours after oral administration)
- Vz/F (apparent volume of distribution of the terminal elimination phase after oral administration)(up to 48 hours after oral administration)
- changes in Ecarin clotting time (ECT)(up to 48 hours after drug administration)
- changes in thrombin time (TT)(up to 48 hours after drug administration)
- changes in vital signs (systolic and diastolic blood pressure, pulse rate)(up to 1 month)
- changes in electrocardiogram(up to 1 month)
- occurrence of adverse events(up to 1 month)
研究者
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