Healthy
Conditions
Brief summary
1. To investigate the relative bioavailability (BA) of improved tablet formulation candidates to determine which formulation will be developed for use in late Phase II and Phase III clinical trials 2. To investigate the relative BA of the pediatric suspension, compared to the current 1B formulation 3. To investigate the bioequivalence (BE) of BILR 355 BS in two tablet strengths; three 25mg tablets vs. one 75 mg tablet, current 1B formulation
Interventions
DRUGBILR 355 BS /1B, current low dose formulation
DRUGBILR 355 BS /1B, current high dose formulation
DRUGBILR 355 BS - Jet Milled (JM) + Sodium Dodecyl Sulfate (SDS) formulation
DRUGBILR 355 BS - Hammer Milled (HM) + Sodium Dodecyl Sulfate (SDS) formulation
DRUGBILR 355 BS - Suspension low dose
DRUGBILR 355 BS - Suspension high dose
DRUGRitonavir
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 60 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy HIV negative adult male volunteers 2. Age ≥18 and ≤ 60 years 3. BMI ≥18.5 and BMI ≤29.9 kg/m2 4. Ability to give signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local regulations
Exclusion criteria
1. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders 2. Surgery of gastrointestinal tract (except appendectomy) 3. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders 4. History of relevant orthostatic hypotension, fainting spells or blackouts 5. Chronic or relevant acute infections 6. History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator 7. Intake of drugs with a long half-life (\>24 hours) within at least one month prior to study drug administration and during the trial 8. Use of drugs within 10 days prior to administration or during the trial which might reasonably influence the results of the trial 9. Participation in another trial with an investigational drug within two months prior to administration or during the trial 10. Current smoker 11. Alcohol abuse (more than 60 g/day) 12. Drug abuse (positive urine test for illicit prescription or non-prescription drugs or drugs of abuse). 13. Blood donation (more than 100 mL within four weeks prior to study drug administration or during the trial) 14. Excessive physical activities (within one week prior to study drug administration or during the trial) 15. Any laboratory value outside the reference range that is of clinical relevance at screening, according to the judgment of the investigator 16. Inability to comply with dietary regimen required by the protocol 17. Infected with hepatitis B or hepatitis C viruses (defined as either being hepatitis B surface antigen, or hepatitis C antibody positive
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | Up to 96 hours after drug administration |
| Cmax (maximum measured concentration of analyte in plasma) | Up to 96 hours after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| λz (terminal rate constant in plasma) | Up to 96 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | Up to 96 hours after drug administration |
| MRTpo (mean residence time of the analyte in the body after po administration) | Up to 96 hours after drug administration |
| CL/F (apparent clearance of the analyte in the plasma after extravascular administration) | Up to 96 hours after drug administration |
| AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point) | Up to 96 hours after drug administration |
| Number of participants with clinically significant changes in vital signs | Up to day 43 after first drug administration |
| Number of participants with abnormal changes in clinical laboratory parameters | Up to day 43 after first drug administration |
| Number of participants with Adverse Events | Up to day 43 after first drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | Up to 96 hours after drug administration |
| tmax (time from dosing to the maximum concentration of the analyte in plasma) | Up to 96 hours after drug administration |
Outcome results
None listed