Bioavailability of BIBR 953 ZW After BIBR 1048 (Oral Pro-drug of BIBR 953 ZW) Administered as Hydroxypropyl Methylcellulose (HPMC) Polymorph II Capsule Relative to HPMC Polymorph I Capsule in Healthy Subjects.

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: BIBR 1048 MS polymorph I; Drug: BIBR 1048 MS polymorph II

• Registration Number: NCT02170974
• Lead Sponsor: Boehringer Ingelheim

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

Detailed Description

Not available

Study Timeline

• Study Start: 2004-07
• Primary Completion: 2004-08
• 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: All
• Target Recruitment: 28

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

Read More

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

Read More

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
BIBR 1048 MS polymorph I	BIBR 1048 MS polymorph I	-
BIBR 1048 MS polymorph II	BIBR 1048 MS polymorph II	-

Primary Outcome Measures

Name	Time	Method
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 Outcome Measures

Name	Time	Method
Changes in systolic and diastolic blood pressure	up to 31 days
Occurrence of adverse events	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
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
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
Assessment of tolerability by investigator on a four-point scale	up to 31 days