Healthy
Conditions
Brief summary
Investigation of the relative bioavailability of BIBR 953 ZW after administration of 150 mg BIBR 1048 polymorph II versus BIBR 953 ZW after administration of 150 mg BIBR 1048 polymorph I in HPMC capsules
Interventions
DRUGBIBR 1048 MS polymorph II
DRUGBIBR 1048 MS polymorph I
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy female and 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
Exclusion criteria
* 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 of more than 400 ml within 4 weeks 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 reference range of clinical relevance * History of any familial bleeding disorder * Platelets \< 150000/μl
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUC0-infinity (area under the plasma concentration-time curve of BIBR 953 ZW from 0 to infinity) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| AUC0-tz | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| Cmax (maximum measured plasma concentration of BIBR 953 ZW) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| CL/F (apparent clearance after oral administration) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| Vz/F (apparent volume of distribution) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| Changes in ECG | up to 31 days |
| tmax (time from dosing to when the plasma concentration reaches Cmax after extravascular doses ) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| Occurrence of adverse events | up to 31 days |
| Assessment of tolerability by investigator on a four-point scale | up to 31 days |
| Changes in systolic and diastolic blood pressure | up to 31 days |
| t1/2 (half life) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
| MRTpo (mean time of residence of drug molecules in the body) | 0 h (predose), 30 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 24 h, 48 h, and 72 h after drug administration |
Outcome results
None listed