Healthy
Conditions
Brief summary
To assess the pharmacokinetics of midazolam with/without concomitant administration of crobenetine
Interventions
DRUGMidazolam, tablet
DRUGCrobenetine, i.v. infusion
DRUGPlacebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Primary purpose
TREATMENT
Masking
SINGLE
Eligibility
Sex/Gender
MALE
Age
21 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
\- All participants in the study should be healthy males, range from 21 to 50 years of age and their bodymass index (BMI) be within 18.5 to 29.9 kg/m2
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * 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 allergy/hypersensitivity (including drug allergy), which is deemed relevant to the trial as judged by the investigator * Intake of drugs with a long half-life (\> 24 hours) within at least one month or less than ten half-lives of the respective drug before enrolment in the study (except substitution therapy regarding thyroid gland) * Use of any drugs that might influence the results of the trial (within one week prior to administration or during the trial) * Participation in another trial with an investigational drug (within two months prior to administration or during the trial) * Smoker (\> 10 cigarettes or \> 3 cigars or \> 3 pipes/day) * Inability to refrain from smoking on trial days * Alcohol abuse (\> 60 g/day) * Drug abuse * Blood donation (≥ 100 mL, within four weeks prior to administration or during the trial) * Excessive physical activities (within the last week before the study) * Any laboratory value outside the reference range of clinical relevance
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the concentration-time curve of midazolam from zero time extrapolated to infinity (AUC0-infinity) | up to 24 hours after start of drug administration |
| Maximum observed concentration of midazolam in plasma (Cmax) | up to 24 hours after start of drug administration |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Time to maximum observed concentration (tmax) | up to 24 hours after start of drug administration | — |
| Individual time courses of plasma concentrations | up to 24 hours after start of drug administration | — |
| Terminal rate constant in plasma (λz) | up to 24 hours after start of drug administration | — |
| Mean residence time in the body (MRT) | up to 24 hours after start of drug administration | — |
| Apparent clearance in plasma (CL/F) | up to 24 hours after start of drug administration | — |
| Volume of distribution (V) | up to 24 hours after start of drug administration | — |
| Terminal half-life in plasma (t1/2) | up to 24 hours after start of drug administration | — |
| Number of patients with clinically relevant findings in vital signs | up to day 8 after drug administration | blood pressure, pulse rate |
| Number of patients with clinically relevant findings in 12-lead ECG | up to day 8 after drug administration | — |
| Number of patients with clinically relevant findings in laboratory tests | up to day 8 after drug administration | — |
| Number of patients with adverse events | up to day 8 after drug administration | — |
| Global assessment of tolerability by the investigator on a 4-point rating scale | up to 192 hours after start of drug administration | — |
| Changes from baseline in physical examination | pre-dose and day 8 after drug administration | — |
| Area under the concentration-time curve (AUC) | up to 24 hours after start of drug administration | — |
Outcome results
None listed