Bioavailability of BIBR 963 ZW After 50 mg of BIBR 1048 MS With and Without of Pantoprazole in Healthy Subjects

Bioavailability of BIBR 953 ZW After 50 mg of BIBR 1048 MS (Oral Prodrug of BIBR 953) in 4 Experimental Formulations Relative to Drinking Solution of BIBR 1048 MS, Each Treatment Given Bid Over 3 Days, in Healthy Subjects. Intraindividual Comparison (5-way Crossover), Randomised, Open. For Each of the 5 Treatments, Investigation of 2 Conditions: With and Without Pantoprazole (Intraindividual, Open Comparison).

To assess the amount of BIBR 953 ZW in urine of 50 mg of BIBR 1048 bid over three days each administered as four experimental capsule formulations relative to drinking solution with and without coadministration of 40 mg pantoprazole.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Pantoprazole; Drug: BIBR 1048 MS Capsule A; Drug: BIBR 1048 MS Capsule B; Drug: BIBR 1048 MS Capsule C; Drug: BIBR 1048 MS Capsule D; Drug: BIBR 1048 MS tartaric acid solution

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 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 (Good Clinical Practice) and local legislation
• Age >= 18 and <= 55 years
• Body Mass Index (BMI) >= 18.5 and <= 29.9 kg/m²

Exclusion Criteria:

• Any finding at the medical examination (including blood pressure, pulse rate and ECG (electrocardiogram)) deviation 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
• History of any bleeding disorder including prolonged or habitual bleeding
• History of other hematologic disease
• History of cerebral bleeding (e.g. after a car accident)
• History of commotio cerebri
• Intake of drug 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 (> 60g/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 Assignment
• Masking: None (Open Label)

Number of Arms

8

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Period 1: BIBR1048 MS Capsule A+Pantoprazole	Drug: Pantoprazole; Drug: BIBR 1048 MS Capsule A
Experimental: Period 1: BIBR1048 MS Capsule B+Pantoprazole	Drug: Pantoprazole; Drug: BIBR 1048 MS Capsule B
Experimental: Period 1: BIBR1048 MS Capsule C+Pantoprazole	Drug: Pantoprazole; Drug: BIBR 1048 MS Capsule C
Experimental: Period 1: BIBR1048 MS Capsule D+Pantoprazole	Drug: Pantoprazole; Drug: BIBR 1048 MS Capsule D
Active Comparator: Period 1: BIBR1048 MS solution+Pantoprazole	Drug: Pantoprazole; Drug: BIBR 1048 MS tartaric acid solution
Experimental: Period 2: BIBR1048 MS Capsule C	Drug: BIBR 1048 MS Capsule C
Experimental: Period 2: BIBR1048 MS Capsule D	Drug: BIBR 1048 MS Capsule D
Active Comparator: Period 2: BIBR1048 MS solution	Drug: BIBR 1048 MS tartaric acid solution

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Ae 0-12h: amount of drug (total BIBR 953 ZW) excreted into urine during all individual dosing intervals	up to 3 days after each administration
Area under the concentration time course at steady state (AUCss)	0.5, 1, 1.5, 2, 4, 6, 8 and 12 hours after study drug administration on day 3 of period 2

Secondary Outcome Measures

Outcome Measure	Time Frame
Occurence of adverse events	up to 40 days
Maximum plasma concentration at steady state (Cmax,ss)	0.5, 1, 1.5, 2, 4, 6, 8 and 12 hours after study drug administration on day 3 of period 2
Time at which maximum plasma concentration occurs after dosing during steady state (tmax,ss)	0.5, 1, 1.5, 2, 4, 6, 8 and 12 hours after study drug administration on day 3 of period 2

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: October 1, 2001
• Primary Completion (Actual): December 1, 2001

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; Gastrointestinal Agents; Protease Inhibitors; Antithrombins; Serine Proteinase Inhibitors; Anticoagulants; Anti-Ulcer Agents; Proton Pump Inhibitors; Dabigatran; Pantoprazole
• Other Study ID Numbers: 1160.31