Oral Bioavailability of Bilastine (BIOBI)

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Faes Farma, S.A.
ClinicalTrials.gov Identifier:
NCT01124123
First received: May 13, 2010
Last updated: September 25, 2012
Last verified: September 2012
  Purpose

The purpose of this study is to assess the absolute bioavailability of an oral bilastine formulation (test drug) compared to the endovenous administration of an IV bilastine formulation (control drug) in healthy volunteers.


Condition Intervention Phase
Healthy
Drug: Bilastine
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Bio-availability Study
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Basic Science
Official Title: Study to Assess Oral Bioavailability of Bilastine (Estudio de Biodisponibilidad Oral de Bilastina)

Further study details as provided by Faes Farma, S.A.:

Primary Outcome Measures:
  • The area under the plasma concentration versus time curve from time zero to infinity (AUC 0-∞ ). [ Time Frame: 17 blood draws performed at: 0,25 - 0,5- 0,75 - 1 - 1,25 - 1,5 - 1,75 - 2 - 2,5 - 3 - 4 - 5 - 7 - 12 - 24 - 48 and 72 hours post administration. ] [ Designated as safety issue: No ]
    Bilastine bioavailability will be obtained from the oral AUC 0-∞ / endovenous AUC 0-∞ quotient.


Secondary Outcome Measures:
  • Additional pharmacokinetic variables: Cmax, AUC 0-t, tmax, Ae, CLr and t ½ [ Time Frame: 17 blood draws and urine collection during 72 hours post administration ] [ Designated as safety issue: No ]
    • Cmax: Maximum plasma concentration; the highest concentration observed during a dosage interval
    • tmax: The time that Cmax was observed
    • AUC 0-t: The area under the plasma concentration versus time curve from time zero to the last time point
    • Ae: amount of accumulated unaltered drug in urine till the last time point
    • Clr: Renal clearance
    • t ½: Elimination halflife

  • Safety and tolerability of a single dose administration of oral and endovenous bilastine [ Time Frame: A last Follow up visit will be performed 7 days after last drug intake ] [ Designated as safety issue: Yes ]
    Safety will be assessed during the study by monitoring adverse events (AEs), clinical laboratory test results (urinalysis, blood chemistry, and haematology), vital signs (including blood pressure, respiration, temperature, and heart rate, supine and standing), electrocardiogram (ECG) results, and abnormal findings upon physical examination.


Enrollment: 12
Study Start Date: May 2010
Study Completion Date: September 2010
Primary Completion Date: June 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Bilastine 20 mg
Single dose 20 mg bilastine oral tablet. Test drug
Drug: Bilastine
20 mg oral tablet
Active Comparator: Bilastine 10 mg
Single dose 10 mg Bilastine endovenous. Control drug
Drug: Bilastine
10 mg endovenous bilastine

Detailed Description:

Single centre, open label, cross-over, randomised, controlled, single dose study. The primary endpoint is the determination of plasma concentrations versus time (17 samples per subject at various time intervals after dosing) in order to assess the oral bioavailability of bilastine in healthy volunteers. Therefore the primary pharmacokinetic variable will be the area under the plasma concentration versus time curve from time zero to infinity (AUC 0-∞). Additionally the following pharmacokinetic variables will also be assessed: Cmax, AUC 0-t, tmax, Ae, Clr, t1/2. Additional objectives are to describe the safety and tolerability of a single administration of oral and endovenous bilastine in healthy volunteers.

Twelve healthy volunteers will be included. Each volunteer will take in random order one single dose of 20 mg oral bilastine and 10 mg IV bilastine with a minimum washout period of 14 days between them.

Bilastine plasma concentrations will be measured using a liquid chromatography/mass mass spectrometry (LC/MS/MS) micro method

  Eligibility

Ages Eligible for Study:   18 Years to 35 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Healthy volunteers of either sex aged from ≥ 18 to ≤ 35 years of age.
  • Body mass index between 19 and 29 Kg/m2.
  • Non smokers.
  • Judged to be in general good health based on medical history, physical examination and clinical laboratory tests.
  • Able to communicate well with the investigator and to comply with the requirements of the entire study.
  • Provision of written informed consent to participate.

Exclusion Criteria:

  • Pregnant or breast-feeding women or with a positive pregnancy test. Subjects who do not agree to use an adequate method of contraception during the study.
  • Intake of another investigational medication in another clinical study within 4 months prior to the first study drug intake.
  • Regular use of any prescribed medication including medicinal herbs or OTC medication within 4 weeks of dosing.
  • A QTc> 430 ms in males and a QTc> 450 ms in females. A HR <55 bpm.
  • Existence of any surgical or medical condition which, in the judgement of the investigator, might interfere with the absorption, distribution, metabolism or excretion of the IMP.
  • Known allergy/hypersensitivity to the study drug or its inactive ingredients.
  • Any clinical conditions or circumstances that in the opinion of the investigator would make the subject unsuitable for the study (e.g., hepatic impairment, renal impairment, mental impairment, cardiac disease).
  • Presence of hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV Ab) or HIV 1 or HIV 2 antibodies at screening.
  • Subjects who have taken metabolic or transporter inducers/inhibitors during the 3 months prior to inclusion in the study.
  • Donation or loss of greater than 200 mL of blood within 12 weeks before entry to the study.
  • Blood transfusion within the prior 6 months to inclusion.
  • Ingestion of citrus fruits and cranberries or any fruit juice within 7 days prior to first dose of study medication.
  • Known current alcohol or drug abuse.
  • Excessive consumption of xanthine containing foods or drinks.
  • Mentally disabled subjects or subjects who by official order have been institutionalised must be excluded from participation.
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01124123

Locations
Spain
Unidad de Investigacion Clinica. Clinica Universidad de Navarra
Pamplona, Navarra, Spain, 31008
Sponsors and Collaborators
Faes Farma, S.A.
Investigators
Principal Investigator: Belen Sadaba, MD Unidad de Investigacion Clinica. Clinica Universidad Navarra (CUN)
  More Information

Additional Information:
Publications:
Additional publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
Responsible Party: Faes Farma, S.A.
ClinicalTrials.gov Identifier: NCT01124123     History of Changes
Other Study ID Numbers: BILA 2909/BA, 2010-019049-25
Study First Received: May 13, 2010
Last Updated: September 25, 2012
Health Authority: Spain: Spanish Agency of Medicines

Keywords provided by Faes Farma, S.A.:
Pharmacokinetics
Oral bioavailability
absorption
AUC
Bioequivalence
Bioavailability study

ClinicalTrials.gov processed this record on April 15, 2014