Bioavailability of BIBR 953 ZW After Administration of BIBR 1048 MS in Healthy Subjects

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: BIBR 1048 MS Capsule I; Drug: BIBR 1048 MS Capsule K; Drug: Pantoprazole; Drug: BIBR 1048 MS drinking solution

• Registration Number: NCT02170623
• Lead Sponsor: Boehringer Ingelheim

Brief Summary

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.

Detailed Description

Not available

Study Timeline

• Study Start: 2002-02
• Primary Completion: 2002-04
• Status Verified: 2014-06
• Study First Submitted: 2014-06-20
• Study First Submitted QC: 2014-06-20
• Last Update Submitted: 2014-06-20
• Study First Posted: 2014-06-23
• Last Update Posted: 2014-06-23

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 12

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 ≤ 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 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 & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Period 1: BIBR 1048 MS with Pantoprazole	BIBR 1048 MS Capsule I	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence. 1. BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days); 2. BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days); 3. BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
Period 1: BIBR 1048 MS with Pantoprazole	BIBR 1048 MS Capsule K	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence. 1. BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days); 2. BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days); 3. BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
Period 1: BIBR 1048 MS with Pantoprazole	BIBR 1048 MS drinking solution	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence. 1. BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days); 2. BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days); 3. BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)
Period 2: BIBR 1048 MS	BIBR 1048 MS Capsule K	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) without Pantoprazole. Fixed sequence. 1. BIBR 1048 MS Capsule K (bid for 3 days); 2. BIBR 1048 MS Drinking solution (bid for 3 days)
Period 2: BIBR 1048 MS	BIBR 1048 MS drinking solution	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) without Pantoprazole. Fixed sequence. 1. BIBR 1048 MS Capsule K (bid for 3 days); 2. BIBR 1048 MS Drinking solution (bid for 3 days)
Period 1: BIBR 1048 MS with Pantoprazole	Pantoprazole	Three treatments of different formulations of 50 mg BIBR 1048 MS (bid for 3 days) with 40 mg Pantoprazole (bid). Randomised sequence. 1. BIBR 1048 MS Capsule I with pantoprazole (bid for 3 days); 2. BIBR 1048 MS Capsule K with pantoprazole (bid for 3 days); 3. BIBR 1048 MS Drinking solution with Pantoprazole (bid for 3 days)

Primary Outcome Measures

Name	Time	Method
Total amount of BIBR 953 ZW excreted into urine during one dosing interval (Ae0-12)	Day 1 to day 10
AUCss (Area under the plasma concentration-time curve 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

Secondary Outcome Measures

Name	Time	Method
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