Bioavailability of BIBR 953 ZW After 50 mg of BIBR 1048 MS (Oral Prodrug of BIBR 953) in 2 Experimental Formulations Relative to Drinking Solution of BIBR 1048 MS, Each Treatment Given Bid Over 3 Days in Healthy Subjects. Intraindividual Comparison (3-way Crossover) With and Without Pantoprazole, Randomised, Open.
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 12
- 主要终点
- Total amount of BIBR 953 ZW excreted into urine during one dosing interval (Ae0-12)
研究概览
简要总结
Study to assess the amount of BIBR 953 ZW in urine and concentrations in plasma after administration of 50 mg of BIBR 1048 bid over three days each administered as two experimental formulations relative to drinking solution with and without coadministration of 40 mg Pantoprazole.
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
- None
入排标准
- 年龄范围
- 18 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 in accordance with GCP and local legislation
- •Age ≥ 18 and ≤ 55 years
- •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
- •History of or current 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)
- •commotio cerebri
- •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 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
Period 1: BIBR 1048 MS with Pantoprazole
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence.
- BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days);
- BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days);
- BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
干预措施: BIBR 1048 MS Capsule I (Drug)
Period 1: BIBR 1048 MS with Pantoprazole
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence.
- BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days);
- BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days);
- BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
干预措施: BIBR 1048 MS Capsule K (Drug)
Period 1: BIBR 1048 MS with Pantoprazole
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence.
- BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days);
- BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days);
- BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
干预措施: Pantoprazole (Drug)
Period 1: BIBR 1048 MS with Pantoprazole
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence.
- BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days);
- BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days);
- BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
干预措施: BIBR 1048 MS drinking solution (Drug)
Period 2: BIBR 1048 MS
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) without Pantoprazole. Fixed sequence.
- BIBR 1048 MS Capsule K (bid for 3 days);
- BIBR 1048 MS Drinking solution (bid for 3 days)
干预措施: BIBR 1048 MS Capsule K (Drug)
Period 2: BIBR 1048 MS
Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) without Pantoprazole. Fixed sequence.
- BIBR 1048 MS Capsule K (bid for 3 days);
- BIBR 1048 MS Drinking solution (bid for 3 days)
干预措施: BIBR 1048 MS drinking solution (Drug)
结局指标
主要结局
Total amount of BIBR 953 ZW excreted into urine during one dosing interval (Ae0-12)
时间窗: Day 1 to day 10
AUCss (Area under the plasma concentration-time curve at steady state) of BIBR 953 ZW
时间窗: 0.5, 1, 1.5, 2, 4, 6, 8, 12 hours after administration of study drug on day 3 of second treatment period
次要结局
- Cmax,ss (maximum concentration at steady state) of BIBR 953 ZW(0.5, 1, 1.5, 2, 4, 6, 8, 12 hours after administration of study drug on day 3 of second treatment period)
- tmax,ss (time from dosing to Cmax at steady state) of BIBR 953 ZW(0.5, 1, 1.5, 2, 4, 6, 8, 12 hours after administration of study drug on day 3 of second treatment period)