Bioavailability of BIBR 1048 MS Tablets in Healthy Subjects With or Without Food

Relative Bioavailability of 200 mg Film Coated Tablets of BIBR 1048 MS With or Without Food Compared to 200 mg Solution of BIBR 1048 MS Given as Single Oral Administrations to Healthy Subjects. A 3-way Crossover, Open, Partly Randomized Study.

Comparative pharmacokinetics of BIBR 1048 MS solution and tablet with or without food

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: BIBR 1048 MS tablet; Drug: BIBR 1048 MS solution

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• 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%

Exclusion Criteria:

• 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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Sequence 1; BIBR 1048 MS tablet (fasted) - BIBR 1048 MS solution (fasted) - BIBR 1048 MS tablet after high fat meal	Drug: BIBR 1048 MS tablet; Drug: BIBR 1048 MS solution
EXPERIMENTAL: Sequence 2; BIBR 1048 MS solution (fasted) - BIBR 1048 MS tablet (fasted) - BIBR 1048 MS tablet after high fat meal	Drug: BIBR 1048 MS tablet; Drug: BIBR 1048 MS solution

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the curve (AUC) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Maximum plasma concentration (Cmax) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Time from dosing to the maximum concentration (tmax) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug

Secondary Outcome Measures

Outcome Measure	Time Frame
Change in activated partial thromboplastin time (aPTT)	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Change in international normalized ratio (INR)	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Terminal half-life (t1/2 ) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Total mean residence time (MRTtot) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Total clearance (CL/f) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug
Volume of distribution (Vz/F) of BIBR 953 ZW	Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 and 48 hours after administration of study drug

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: July 1, 1999
• Primary Completion (ACTUAL): August 1, 1999

Study Registration Dates

• First Submitted: June 20, 2014
• First Submitted That Met QC Criteria: June 20, 2014
• First Posted (ESTIMATE): June 23, 2014

Study Record Updates

• Last Update Posted (ESTIMATE): June 23, 2014
• Last Update Submitted That Met QC Criteria: June 20, 2014
• Last Verified: June 1, 2014

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protease Inhibitors; Antithrombins; Serine Proteinase Inhibitors; Anticoagulants; Dabigatran
• Other Study ID Numbers: 1160.3