Healthy
Conditions
Brief summary
Study to determine the relative bioavailability of 500/200 mg of tipranavir/ritonavir (TPV/r) oral solution compared to 500/200 mg of TPV/r capsules following oral administration and to investigate the relative bioavailability of 500/200 mg of TPV/r oral solution with food versus without food.
Interventions
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy males and females according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs (BP, HR), 12-lead ECG, clinical laboratory tests * No finding deviating from normal and of clinical relevance * No evidence of a clinically relevant concomitant disease 2. Age ≥ 18 and Age ≤ 55 years 3. BMI ≥ 18.5 and BMI ≤ 29.9 kg/m2 (Body Mass Index) 4. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation
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 or less than 10 half-lives of the respective drug prior to administration or during the trial 8. Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial (e.g. drugs which contain polyethylene glycol or vitamin E) 9. Participation in another trial with an investigational drug within two months prior to administration or during the trial 10. Smoker (more than 10 cigarettes/day or 3 cigars/day or 3 pipes/day) 11. Inability to refrain from smoking on trial days 12. Alcohol abuse (more than 60 g/day) 13. Drug abuse 14. Veins unsuited for iv puncture on either arm (e.g. veins which are difficult to locate, access or puncture, veins with a tendency to rupture during or after puncture) 15. Blood donation (more than 100 mL within four weeks prior to administration or during the trial) 16. History of any bleeding disorder or acute blood coagulation defect of vitamin K deficiency caused by anticoagulation therapy or malabsorption 17. Vitamin E supplement intake 18. Excessive physical activities (within one week prior to administration or during the trial) 19. Any laboratory value outside the reference range that is of clinical relevance 20. Inability to comply with dietary regimen of study centre For female subjects: 21. Pregnancy 22. Positive pregnancy test 23. No adequate contraception e.g. oral contraceptives, sterilization, intrauterine device 24. Inability to maintain this adequate contraception during the whole study period 25. Lactation period
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Cmax (maximum concentration of tipranavir in plasma) | up to 72 hours after drug administration |
| AUC0-∞ (area under the concentration time curve of tipranavir in plasma over the time interval from 0 extrapolated to infinity) | up to 72 hours after drug administration |
Secondary
| Measure | Time frame |
|---|---|
| t1/2 (terminal half-life of tipranavir in plasma) | up to 72 hours after drug administration |
| MRTpo (mean residence time of the analyte in the body after oral administration) | up to 72 hours after drug administration |
| AUC0-tz (area under the concentration-time curve of tipranavir in plasma over the time interval from 0 to the time of the last quantifiable data point) | up to 72 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | up to 72 hours after drug administration |
| Number of subjects with adverse events | up to day 18 |
| CLpo/F (apparent clearance of tipranavir in the plasma after extravascular administration) | up to 72 hours after drug administration |
| tmax (time from dosing to the maximum concentration of tipranavir in plasma) | up to 72 hours after drug administration |
Outcome results
None listed