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Effects of TPV/r on the Pharmacokinetics of Carbamazepine in Healthy Adult Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02253849
Lead Sponsor
Boehringer Ingelheim
Brief Summary

Study to assess the steady-state pharmacokinetics of carbamazepine (CBZ) at 200 mg or 100 mg twice daily, depending on tolerability, and administered alone and in combination with tipranavir/ritonavir (TPV/r) after a single dose (500/200 mg) and at steady-state (500/200 mg twice-daily)

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
28
Inclusion Criteria
  • Healthy male and non-pregnant, non-lactating female subjects as determined by results of screening
  • Signed written informed consent in accordance with Good Clinical Practice (GCP) and local legislation
  • The ability to understand and sign a written informed consent form, prior to participation in any screening procedures and must be willing to comply with all study requirements
  • Age >19 and <59 years
  • Weight ≥ 60 kg
  • BMI >18.5 and <35 kg/m2
  • Ability to maintain adequate contraception if applicable
Exclusion Criteria
  • Any finding of the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance
  • AV block including 1°
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, haematological, oncological or hormonal disorders
  • Surgery of gastrointestinal tract (except appendectomy)
  • Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
  • Relevant history of 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
  • Known hypersensitivity to TPV, Ritonavir (RTV), carbamazepine or antiretroviral drugs (marketed or experimental use as part of clinical research studies)
  • Known elevated liver enzymes in past trials with any compound
  • Intake of drugs with a long half-life (>24 hours) (<1 month prior to administration or during the trial)
  • Prescription or over the counter medications (including vitamins, minerals, herbal supplements and antacids), dietary supplements 14 days prior to study drug administration or expected during the trial)
  • Participation in another trial with an investigational drug (<2 months prior to administration or expected during trial)
  • Smoker with a consumption of >10 cigarettes or >3 cigars or >3 pipes/day and those who cannot keep tobacco intake constant
  • Alcohol abuse (>60 g/day)
  • Drug abuse
  • Blood donation or loss >400 mL, <1 month prior to administration or expected during the trial
  • Clinically relevant laboratory abnormalities
  • Inability to comply with dietary regimen of study centre

For female subjects:

  • Pregnancy or planning to become pregnant within 60 days of study completion
  • Positive pregnancy test
  • Have not been using a barrier method of contraception for at least 3 months prior to participation in the study
  • Are not willing or are unable to use a reliable method of barrier contraception (such as diaphragm with spermicidal cream/jelly or condoms with spermicidal foam), during and up to 2 months after completion/termination of the trial
  • Chronic use of oral contraception or hormone replacement containing ethinyl estradiol
  • Breast-feeding

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
CBZ - TPB/r+CBZTipranavirDays 1-14: carbamazepine (CBZ) twice daily Days 15-22: CBZ twice daily plus TPV/r twice daily
CBZ - TPB/r+CBZCarbamazepineDays 1-14: carbamazepine (CBZ) twice daily Days 15-22: CBZ twice daily plus TPV/r twice daily
CBZ - TPB/r+CBZRitonavirDays 1-14: carbamazepine (CBZ) twice daily Days 15-22: CBZ twice daily plus TPV/r twice daily
Primary Outcome Measures
NameTimeMethod
Area under the concentration-time curve of Carbamazepine in plasma over the time interval t0h to t12h (AUC0-12h)up to 12 hours after drug administration
Maximum measured concentration of Carbamazepine in plasma (Cmax)up to 12 hours after drug administration
Drug concentration of Carbamazepine in plasma at 12 hours after drug administration (Cp12h)up to 12 hours after drug administration
Secondary Outcome Measures
NameTimeMethod
AUC0-12hup to 12 hours after drug administration
Cmaxup to 12 hours
Cp12hup to 12 hours after drug administration
Clearance (CL/F)up to 12 hours after drug administration
Volume of distributionup to 12 hours after drug administration
Time from dosing to the maximum concentration (Tmax)up to 12 hours after drug administration
t1/2 (terminal elimination half-life)up to 12 hours after drug administration
Number of subjects with adverse eventsup to 35 days
Number of subjects with clinically relevant changes in laboratory parametersup to 35 days
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