Study of New Tablet Formulations and Suspension Formulation Compared to Current (1B) Formulation of BILR 355 BS in Healthy Male Volunteer Subjects

NCT02259868 | Completed Phase 1

• 1 other identifier: 1188.5
• Study Type: interventional
• Target: 88
• Locations: 0 countries
• Sites: N/A

Brief Summary

1. 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. 2.To investigate the relative BA of the pediatric suspension, compared to the current 1B formulation
3. 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

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• 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 Outcomes (10)

• 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

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

  Up to 96 hours after drug administration

• 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

Study Arms (4)

Group A

EXPERIMENTAL

randomized sequence of current low dose formulation (3 tablets) and high dose (1 tablet) BILR 355 BS 1B formulation, separated by 14-day washout

Drug: BILR 355 BS /1B, current low dose formulation; Drug: BILR 355 BS /1B, current high dose formulation; Drug: Ritonavir

Group B

EXPERIMENTAL

randomized sequence of BILR 355 BS (JM) + SDS formulation low dose (2 tablets) ,BILR 355 BS (HM) + SDS formulation low dose (2 tablets), BILR 355 BS high dose 1B formulation (4 low dose tablets), separated by 14-day washout

Drug: BILR 355 BS /1B, current low dose formulation; Drug: BILR 355 BS - Jet Milled (JM) + Sodium Dodecyl Sulfate (SDS) formulation; Drug: BILR 355 BS - Hammer Milled (HM) + Sodium Dodecyl Sulfate (SDS) formulation; Drug: Ritonavir

Group C

EXPERIMENTAL

randomized sequence of BILR 355 BS (JM) + SDS formulation high dose (4 tablets) , BILR 355 BS (JM) + SDS formulation mid dose (3 tablets), BILR 355 BS (HM) + SDS formulation high dose (4 tablets), separated by 14-day washout

Drug: BILR 355 BS - Jet Milled (JM) + Sodium Dodecyl Sulfate (SDS) formulation; Drug: BILR 355 BS - Hammer Milled (HM) + Sodium Dodecyl Sulfate (SDS) formulation; Drug: Ritonavir

Group D

EXPERIMENTAL

randomized sequence of BILR 355 BS Suspension high dose, BILR 355 BS Suspension low dose, current low dose BILR 355 BS 1B formulation (3 tablets) separated by 14-day washout

Drug: BILR 355 BS /1B, current low dose formulation; Drug: BILR 355 BS - Suspension low dose; Drug: BILR 355 BS - Suspension high dose; Drug: Ritonavir

Interventions

BILR 355 BS /1B, current low dose formulation DRUG

Group A; Group B; Group D

BILR 355 BS /1B, current high dose formulation DRUG

Group A

BILR 355 BS - Jet Milled (JM) + Sodium Dodecyl Sulfate (SDS) formulation DRUG

Group B; Group C

BILR 355 BS - Hammer Milled (HM) + Sodium Dodecyl Sulfate (SDS) formulation DRUG

Group B; Group C

BILR 355 BS - Suspension low dose DRUG

Group D

BILR 355 BS - Suspension high dose DRUG

Group D

Ritonavir DRUG

Group A; Group B; Group C; Group D

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy HIV negative adult male volunteers
• Age ≥18 and ≤ 60 years
• BMI ≥18.5 and BMI ≤29.9 kg/m2
• 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

You may not qualify if:

• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of 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 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 prior to study drug administration and during the trial
• Use of drugs within 10 days prior to administration or during the trial which might reasonably influence the results of the trial
• Participation in another trial with an investigational drug within two months prior to administration or during the trial
• Current smoker
• Alcohol abuse (more than 60 g/day)
• Drug abuse (positive urine test for illicit prescription or non-prescription drugs or drugs of abuse).
• Blood donation (more than 100 mL within four weeks prior to study drug administration or during the trial)
• Excessive physical activities (within one week prior to study drug administration or during the trial)
• Any laboratory value outside the reference range that is of clinical relevance at screening, according to the judgment of the investigator

Sponsors & Collaborators

• Boehringer Ingelheim: lead

MeSH Terms

Interventions

Dosage Forms; Sodium Dodecyl Sulfate; Ritonavir

Intervention Hierarchy (Ancestors)

Pharmaceutical Preparations; Technology, Pharmaceutical; Investigative Techniques; Dodecanol; Fatty Alcohols; Alcohols; Organic Chemicals; Alkanesulfonates; Alkanesulfonic Acids; Sulfonic Acids; Sulfur Acids; Sulfur Compounds; Lipids; Thiazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

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: October 7, 2014
• First Posted: October 9, 2014
• Study Start: June 1, 2005
• Primary Completion: September 1, 2005
• Last Updated: August 31, 2018

Record last verified: 2018-08