Bioavailability of BIBR 1048 MS Single Doses With or Without Pantoprazole in Healthy Subjects

NCT02170805 | Completed Phase 1

• 1 other identifier: 1160.17
• Study Type: interventional
• Target: 24
• Locations: 0 countries
• Sites: N/A

Brief Summary

The pharmacokinetics of 50 mg BIBR 1048 administered as two newly developed capsule formulation using melt extrusion technology was assessed in two separate, single dose, 3-way crossover, open design, randomised studies. The 3-way crossover treatments included administration of the tartaric acid solution of 50 mg BIBR 1048, the capsule formulation A or B and administration of the capsules with coadministration of pantoprazole.

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• AUC0-∞ (Area under the concentration-time curve the time interval from 0 extrapolated to infinity) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

• AUC0-tf (Area under the concentration-time curve over the time interval from 0 to the time of the last quantifiable concentration) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

Secondary Outcomes (9)

• Cmax (Maximum measured concentration) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

• tmax (Time from dosing to the maximum concentration) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

• t1/2 (Terminal half-life) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

• MRTtot (Total mean residence time) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

• CLtot/F (Total apparent clearance) of BIBR 953 ZW

  Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug

Study Arms (2)

Substudy 1

EXPERIMENTAL

Three treatments of single administrations of BIBR 1048 MS 50 mg with or without pantoprazole; randomised sequence 1. BIBR 1048 MS capsule formulation A without pantoprazole; 2. BIBR 1048 MS capsule formulation A with coadministration of 40 mg pantoprazole (bid); 3. BIBR 1048 MS powder plus solution without pantoprazole

Drug: BIBR 1048 MS capsule formulation A; Drug: BIBR 1048 MS powder plus solution; Drug: Pantoprazole

Substudy 2

EXPERIMENTAL

Three treatments of single administrations of BIBR 1048 MS 50 mg with or without pantoprazole; randomised sequence 1. BIBR 1048 MS capsule formulation B without pantoprazole; 2. BIBR 1048 MS capsule formulation B with coadministration of 40 mg pantoprazole (bid); 3. BIBR 1048 MS powder plus solution without pantoprazole

Drug: BIBR 1048 MS capsule formulation B; Drug: BIBR 1048 MS powder plus solution; Drug: Pantoprazole

Interventions

BIBR 1048 MS capsule formulation A DRUG

BIBR 1048 MS, formulation A 50 mg

Substudy 1

BIBR 1048 MS capsule formulation B DRUG

BIBR 1048 MS, formulation B 50 mg

Substudy 2

BIBR 1048 MS powder plus solution DRUG

BIBR 1048 MS, powder plus solution 50 mg

Substudy 1; Substudy 2

Pantoprazole DRUG

Pantoprazole 40 mg

Also known as: Pantozol®

Substudy 1; Substudy 2

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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
• Broca ≥ - 20% and ≤ + 20%

You may not qualify if:

• 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)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Solutions; Pantoprazole

Intervention Hierarchy (Ancestors)

Pharmaceutical Preparations; 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 20, 2014
• First Posted: June 23, 2014
• Study Start: April 1, 2001
• Primary Completion: June 1, 2001
• Last Updated: June 23, 2014

Record last verified: 2014-06