NCT02171000已完成1 期
Safety, Pharmacokinetics and Pharmacodynamics After Multiple Oral Doses of BIBR 1048 MS Capsule (150 mg b.i.d., 7 Days) in Healthy Japanese Male Subjects (Open Label 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
- 7
- 主要终点
- Change from baseline in physical examination
研究概览
简要总结
To investigate safety, pharmacokinetics and pharmacodynamics of BIBR 1048 MS following oral administration of multiple doses (150 mg b.i.d., 7 days)
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 20 Years 至 35 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subjects according to the following criteria:
- •Based upon a complete medical history, including the physical examination, vital signs (blood pressure, pulse rate and body temperature), 12-lead ECG, clinical laboratory tests
- •1.1 No finding of clinical relevance
- •1.2 No evidence of a clinically relevant concomitant disease
- •Age ≥20 and Age ≤35 years
- •Body Mass Index (BMI) ≥18 and BMI <25 kg/m2 (Body Mass Index)
- •Signed and dated written informed consent prior to admission to the trial in accordance with Japanese GCP (Ministry of Health, Labour and Welfare Ordinance No.28, March 27, 1997).
排除标准
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Subject was not able to use an adequate form of contraception from the time of the first dose on Day 1 up to end-of study examination
- •Diseases of the central nervous system (such as epilepsy), psychiatric disorders or neurological disorders
- •History of clinically significant orthostatic hypotension, clinically significant current or past fainting spells or blackouts.
- •Chronic or relevant acute infections
- •allergy/hypersensitivity (including drug allergy) which was deemed relevant to the safety assessment as judged by the investigator (excluding asymptomatic seasonal rhinitis/hay fever)
- •any bleeding disorder including prolonged or habitual bleeding
- •other hematologic diseases
- •cerebral bleeding (e.g. after a car accident)
- •concussions (head trauma resulting in injuring to brain) with or without loss of consciousness
- •Intake of drugs with a long half-life (> 24 hours) within at least 1 month or less than 10 half-lives, whichever was shorter, of the respective drug prior to administration or during the trial
- •Use of aspirin (including over-the-counter medications), antiplatelet agents like ticlopidine or dipyridamole, chronic administration of non-steroidal anti-inflammatory drugs (NSAIDs, coumadin like anticoagulants, chronic use of corticosteroids, heparin or fibrinolytic agents within 14 days prior to administration up to end-of-study examination
- •Participation in another trial with an investigational drug within 3 months prior to administration up to end-of-study examination
- •Smoker (>10 cigarettes/day or inability to refrain from smoking during the trial)
- •Alcohol abuse (more than 60 g/day; confirmed by interview)
- •Drug abuse (confirmed by interview)
- •Blood donation (more than 100 mL from 3 months prior to screening and any blood donation from screening up to end-of-study examination)
- •Excessive physical activities (within 7 days prior to the first drug administration up to end-of-study examination)
- •Any laboratory value outside the reference range that was of clinical relevance
- •Known hypersensitivity to the investigational drug or its excipients
- •Subject who was judged ineligible by the investigator or the sub-investigator
- •History of any familial bleeding disorder
- •Thrombocytes < 15 x 104 /μL
研究组 & 干预措施
BIBR 1048
Experimental
BIBR 1048 MS
干预措施: BIBR 1048 MS (Drug)
结局指标
主要结局
Change from baseline in physical examination
时间窗: within 14 days prior to drug administration until up to 18 days post drug administration
Change from baseline in vital signs
时间窗: within 14 days prior to drug administration until up to 18 days post drug administration
Change from baseline in 12-lead electrocardiogram (ECG)
时间窗: within 14 days prior to drug administration until up to 18 days post drug administration
Change from baseline in clinical laboratory tests
时间窗: within 14 days prior to drug administration until up to 18 days post drug administration
Number of participants with adverse events
时间窗: within 14 days prior to drug administration until up to 18 days post drug administration
次要结局
- Changes in activated partial thromboplastin time (aPTT)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Changes in ecarin clotting time (ECT)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Changes in thrombin time (TT)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Changes in prothrombin time expressed as international normalised ratio (INR)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Maximum measured concentration of the analyte in plasma (Cmax)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Minimum concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmin,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ (AUCτ,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Terminal rate constant in plasma at steady state (λz,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Terminal half-life of the analyte in plasma at steady state (t1/2,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Mean residence time of the analyte in the body at steady state after po administration (MRTpo,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Apparent clearance of the analyte in the plasma at steady state after extravascular multiple dose administration (CL/F,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Apparent volume of distribution during the terminal phase λz at steady state following extravascular administration (Vz/F,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Renal clearance of the analyte from the time point t1 until the time point t2 (CLR,t1-t2 )(Day 1: 0-4, 4-8, 8-12 and 12-24 hours after the first drug administration, on Day 7: 0-4, 4-8, 8-12, 12-24, 24-48 and 48-72 hours after the last drug administration)
- Time from dosing to maximum measured concentration of the analyte in plasma (tmax)(Day 1 and 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 h after drug administration (morning), Day 2 to 6 prior drug administration (morning), Day 5 and 6 prior drug administration (evening), Day 7 24, 36, 48 h after final drug administration)
- Area under the concentration-time curve of the analyte in plasma over a uniform dosing interval τ after administration of the single dose on Day 1 (AUCτ,1)(Day 1 before, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10 and 12 hours after drug administration in the morning)
- Amount of analyte that is eliminated in urine from the time point t1 to time point t2 ( Aet1-t2 )(Day 1: 0-4, 4-8, 8-12 and 12-24 hours after the first drug administration, on Day 7: 0-4, 4-8, 8-12, 12-24, 24-48 and 48-72 hours after the last drug administration)
- Fraction of analyte eliminated in urine from time point t1 to time point t2 (fet1-t2)(Day 1: 0-4, 4-8, 8-12 and 12-24 hours after the first drug administration, on Day 7: 0-4, 4-8, 8-12, 12-24, 24-48 and 48-72 hours after the last drug administration)
- Maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmax,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Time from last dosing to maximum concentration of the analyte in plasma at steady state (tmax,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
- Amount of analyte that is eliminated in urine at steady state from the time point t1 to time point t2 (Aet1-t2,ss)(Day 7 : 0-4, 4-8, 8-12, 12-24, 24-48 and 48-72 hours after the last drug administration)
- Fraction of analyte eliminated in urine at steady state from time point t1 to time point t2 (fet1-t2,ss)(Day 7: 0-4, 4-8, 8-12, 12-24, 24-48 and 48-72 hours after the last drug administration)
- Renal clearance of the analyte in plasma from the time point t1 until the time point t2 at steady state (CLR,t1-t2,ss)(Day 7 prior, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 hours after final drug administration)
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