Pharmacokinetics of BIBR 953 ZW After 150 mg of BIBR 1048 (Oral Pro-drug of BIBR 953) Administered as Capsule Twice Daily Over Seven Days With or Without Pantoprazole Co-treatment to Healthy Male and Female Elderly Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 36
- 主要终点
- AUCτ,ss (area under the plasma concentration time curve during a dosing interval at steady state)
研究概览
简要总结
To assess the steady state pharmacokinetic profile of BIBR 953 ZW after administration of BIBR 1048 to male and female elderly subjects, to assess pharmacokinetic gender differences. To assess the effect of coadministration of Pantoprazole on the bioavailability of BIBR 953 ZW.
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
- 65 Years 至 —（Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy male and female elderly subjects as determined by results of screening
- •Signed written informed consent in accordance with GCP and local legislation
- •Age ≥ 65, no upper limit
- •BMI ≥ 18.5 and ≤ 29.9 kg/m2
排除标准
- •Any finding at the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
- •Clinically relevant gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
- •History of relevant 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)
- •cranio-cerebral trauma
- •Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
- •Use of any drugs that might influence the results of the trial within 10 days prior to administration or during the 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 intake (>30 - 40 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 < 140000/μl (male) or < 156000/μl (female)
研究组 & 干预措施
BIBR 1048 MS without Pantoprazole
150 mg BIBR 1048 MS capsules administered twice daily over 6 days and once in the morning of the seventh day
干预措施: BIBR 1048 MS (Drug)
BIBR 1048 MS with Pantoprazole
150 mg BIBR 1048 MS capsules administered twice daily over 6 days and once in the morning of the seventh day together with Pantoprazole. Pantoprazole administration (40 mg bid) started two days before administration og BIBR 1048 and ended in the morning of the seventh day.
干预措施: BIBR 1048 MS (Drug)
BIBR 1048 MS with Pantoprazole
150 mg BIBR 1048 MS capsules administered twice daily over 6 days and once in the morning of the seventh day together with Pantoprazole. Pantoprazole administration (40 mg bid) started two days before administration og BIBR 1048 and ended in the morning of the seventh day.
干预措施: Pantoprazole (Drug)
结局指标
主要结局
AUCτ,ss (area under the plasma concentration time curve during a dosing interval at steady state)
时间窗: Day 4 and 7
Cmax,ss (maximum measured concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
时间窗: Day 4 and 7
Aeτ,ss (amount of dose excreted in urine over one dosing interval at steady state)
时间窗: Day 4 and 7
feτ,ss (percent of dose excreted in urine over one dosing interval at steady state)
时间窗: Day 4 and 7
AUC0-tz,ss (area under the plasma concentration time curve (AUC) from zero time (pre dose) to the time of the last quantifiable concentration (tz))
时间窗: Day 4 and 7
Cmin,ss (minimum measured concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
时间窗: Day 4 and 7
tmax,ss (time from last dosing to the maximum concentration of the analyse in plasma at steady state over a uniform dosing interval τ)
时间窗: Day 4 and 7
t½,ss (terminal half-life, calculated from the terminal elimination rate constant)
时间窗: Day 4 and 7
次要结局
- CLR,ss (renal clearance at steady state following multiple dose administration)(Day 4 and 7)
- MRTss (steady state mean residence time)(Day 4 and 7)
- CL/F,ss (apparent clearance of the analyse in plasma at steady state after extravascular multiple dose administration)(Day 4 and 7)
- Vz/F,ss (apparent volume of distribution during the terminal phase at steady state following extravascular administration)(Day 4 and 7)
- Changes in activated partial thromboplastin time (aPTT)(Day 4 and 7)
- Changes in ecarin clotting time (ECT)(Day 4 and 7)
- Occurrence of Adverse Events(up to 10 days)