Bioavailability of Tipranavir/Ritonavir Paediatric Solution Compared to Tipranavir/Ritonavir Capsules in Healthy Female and Male Subjects

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: Tipranavir oral solution; Drug: Tipranavir capsules; Drug: Ritonavir soft gel capsules; Drug: Ritonavir oral solution; Other: High fat breakfast

• Registration Number: NCT02251158
• Lead Sponsor: Boehringer Ingelheim

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.

Detailed Description

Not available

Study Timeline

• Study Start: 2003-10
• Primary Completion: 2003-12
• Status Verified: 2014-09
• Study First Submitted: 2014-09-25
• Study First Submitted QC: 2014-09-25
• Last Update Submitted: 2014-09-25
• Study First Posted: 2014-09-29
• Last Update Posted: 2014-09-29

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 30

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

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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

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
TPV/r	Tipranavir oral solution	Tipranavir/Ritonavir paediatric/oral solution
TPV/r capsules	Tipranavir capsules	-
TPV/r capsules	Ritonavir soft gel capsules	-
TPV/r with food	Ritonavir oral solution	Tipranavir/Ritonavir paediatric/oral solution
TPV/r with food	Tipranavir oral solution	Tipranavir/Ritonavir paediatric/oral solution
TPV/r with food	High fat breakfast	Tipranavir/Ritonavir paediatric/oral solution
TPV/r	Ritonavir oral solution	Tipranavir/Ritonavir paediatric/oral solution

Primary Outcome Measures

Name	Time	Method
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
Cmax (maximum concentration of tipranavir in plasma)	up to 72 hours after drug administration

Secondary Outcome Measures

Name	Time	Method
t1/2 (terminal half-life of tipranavir in plasma)	up to 72 hours after drug administration
CLpo/F (apparent clearance of tipranavir in the plasma after extravascular 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
tmax (time from dosing to the maximum concentration 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
Number of subjects with adverse events	up to day 18
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)	up to 72 hours after drug administration