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Pharmacokinetic Properties of Nevirapine Extended Release Tablets When Administered Orally in Healthy Male Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Nevirapine, low dose
Drug: Nevirapine, high dose
Registration Number
NCT02194218
Lead Sponsor
Boehringer Ingelheim
Brief Summary

Study to determine the pharmacokinetic properties of 200 mg nevirapine (NVP) administered as 4 x 50 mg extended release (XR) tablets in a single dose and to establish the bioequivalence of this formulation compared to 200 mg NVP administered as 2 x 100 mg XR tablets in a single dose

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
48
Inclusion Criteria
  • Healthy male according to the following criteria based upon a complete medical history, including the physical examination, vital signs (Blood Pressure (BP), Pulse Rate (PR)), 12-lead electrocardiogram (ECG), clinical laboratory; values within normal ranges or deviating from normal without clinical relevance as considered by the investigator
  • Age ≥21 and Age ≤50 years
  • Body Mass Index (BMI) ≥18.5 and BMI ≤29.9 kg/m2
  • Signed and dated written informed consent prior to admission to the study in accordance with Good clinical practice (GCP) and the local legislation
Exclusion Criteria
  • Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
  • Any evidence of a clinically relevant concomitant disease
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders of clinical relevance
  • Surgery of the gastrointestinal tract (except appendectomy and herniotomy)
  • 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 relevant allergy/hypersensitivity (including allergy to drug or its excipients)
  • 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
  • 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
  • Participation in another trial with an investigational drug within two months prior to administration or during the trial
  • Previous intake of Nevirapine
  • Smoker (>10 cigarettes or >3 cigars or >3 pipes/day)
  • Inability to refrain from smoking on trial days
  • Alcohol abuse (more than 30 g/day)
  • Drug abuse
  • Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
  • Excessive physical activities (within one week prior to administration or during the trial)
  • Any laboratory value outside the reference range that is of clinical relevance
  • Inability to comply with dietary regimen of trial site

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Nevirapine XR 4 dosesNevirapine, low dose-
Nevirapine XR 2 dosesNevirapine, high dose-
Primary Outcome Measures
NameTimeMethod
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞)up to 144 hours post-dose
Maximum measured concentration of the analyte in plasma (Cmax)up to 144 hours post-dose
Secondary Outcome Measures
NameTimeMethod
Terminal half-life of the analyte in plasma (t1/2)up to 144 hours post-dose
Apparent clearance of the analyte in the plasma after extravascular administration (CL/F)up to 144 hours post-dose
Absorption rate constant (ka)up to 144 hours post-dose
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 (AUC0-tz)up to 144 hours post-dose
Assessment of tolerability by investigator on a 4-point scalewithin 8 days after last trial procedure
Terminal rate constant in plasma (λz)up to 144 hours post-dose
Number of patients with adverse eventsup to 35 days
Time from dosing to the maximum concentration of the analyte in plasma (tmax)up to 144 hours post-dose
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F)up to 144 hours post-dose
Mean residence time of the analyte in the body after po administration (MRTpo)up to 144 hours post-dose
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