Relative Bioavailability of Different Formulations of BI 671800 in Healthy Male and Female Volunteers

NCT02221388 | Completed Phase 1

• 1 other identifier: 1268.56
• Study Type: interventional
• Target: 24
• Locations: 0 countries
• Sites: N/A

Brief Summary

To compare the oral bioavailability and rate of absorption of two different formulations of BI 671800 HEA (choline salt) tablets 200 mg, one with enteric coating (EC) and one without EC, versus 2 x 100 mg BI 671800 ED (ethylenediamine salt) capsules. Both BI 671800 HEA formulations were further investigated concerning food effect and one of the two BI 671800 HEA formulations identified by interim pharmacokinetic analysis was further investigated concerning dose proportionality with 50 mg.

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• Cmax (maximum measured concentration of BI 671800 in plasma)

  Up to 24 hours after last drug administration

• AUC0-∞ (area under the concentration time curve of BI 671800 in plasma over the time interval from 0 extrapolated to infinity)

  Up to 24 hours after last drug administration

Secondary Outcomes (13)

• tmax (time from dosing to the maximum concentration of BI 671800 in plasma)

  Up to 24 hours after last drug administration

• AUC0-tz (area under the concentration-time curve of BI 671800 in plasma over the time interval from 0 to the time of the last quantifiable data point)

  Up to 24 hours after drug administration

• λz (terminal rate constant in plasma)

  Up to 24 hours after drug adminnistration

• t½ (terminal half-life of BI 671800 in plasma)

  Up to 24 hours after drug administration

• MRTpo (mean residence time of BI 671800 in the body after po administration)

  Up to 24 hours after drug administration

Study Arms (6)

BI 671800 ED capsules

ACTIVE COMPARATOR

Drug: BI 671800 ED, 100 mg capsules

BI 671800 HEA tablet in fasted state

EXPERIMENTAL

Drug: BI 671800 HEA, 200 mg tablets

BI 671800 HEA EC tablet in fasted state

EXPERIMENTAL

Drug: BI 671800 HEA EC, 200 mg tablets

BI 671800 HEA tablet in fed state

EXPERIMENTAL

Drug: BI 671800 HEA, 200 mg tablets; Other: Standard meal

BI 671800 HEA EC tablet in fed state

EXPERIMENTAL

Drug: BI 671800 HEA EC, 200 mg tablets; Other: Standard meal

BI 671800 HEA, 50 mg tablet in fasted state

EXPERIMENTAL

Drug: BI 671800 HEA, 50 mg tablets

Interventions

BI 671800 HEA, 200 mg tablets DRUG

BI 671800 HEA tablet in fasted state; BI 671800 HEA tablet in fed state

BI 671800 HEA EC, 200 mg tablets DRUG

BI 671800 HEA EC tablet in fasted state; BI 671800 HEA EC tablet in fed state

BI 671800 HEA, 50 mg tablets DRUG

BI 671800 HEA, 50 mg tablet in fasted state

BI 671800 ED, 100 mg capsules DRUG

BI 671800 ED capsules

Standard meal OTHER

BI 671800 HEA EC tablet in fed state; BI 671800 HEA tablet in fed state

Eligibility Criteria

• Age: 21 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy males and females according to the following criteria: Based upon a complete medical history, including physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests
• Age 21 to 50 years (incl.)
• BMI 18.5 to 29.9 kg/m2 (incl.)
• Signed and dated written informed consent prior to admission to the study in accordance with GCP and the local legislation

You may not qualify if:

• Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
• Any evidence of a clinically relevant concomitant disease
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of the gastrointestinal tract (except appendectomy)
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• History of relevant orthostatic hypotension, fainting spells or blackouts
• Chronic or relevant acute infections
• History of relevant allergy or hypersensitivity (including allergy to drug or its excipients)
• Intake of drugs within one month or less than 10 half-lives of the respective drug prior to first study drug administration
• Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
• Smoker (more than 10 cigarettes or 3 cigars or 3 pipes daily)
• Alcohol abuse (average consumption of more than 20 g/day in females and 30 g/day in males)
• Drug abuse
• Blood donation (more than 100 mL within four weeks prior to day 1 of visit 2)
• Any laboratory value outside the reference range that is of clinical relevance, especially repeated alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyltransferase (GGT), alkaline phosphatase (ALP) or total bilirubin above upper limit of normal (ULN) at screening and not resolved before dosing.

Sponsors & Collaborators

• Boehringer Ingelheim: lead

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: August 19, 2014
• First Posted: August 20, 2014
• Study Start: February 1, 2010
• Primary Completion: July 1, 2010
• Last Updated: August 20, 2014

Record last verified: 2014-08