Oral Bioavailability of Bilastine (BIOBI)
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.
|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)|
- 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.
- 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.
|Study Start Date:||May 2010|
|Study Completion Date:||September 2010|
|Primary Completion Date:||June 2010 (Final data collection date for primary outcome measure)|
Experimental: Bilastine 20 mg
Single dose 20 mg bilastine oral tablet. Test drug
20 mg oral tablet
Active Comparator: Bilastine 10 mg
Single dose 10 mg Bilastine endovenous. Control drug
10 mg endovenous bilastine
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
|Unidad de Investigacion Clinica. Clinica Universidad de Navarra|
|Pamplona, Navarra, Spain, 31008|
|Principal Investigator:||Belen Sadaba, MD||Unidad de Investigacion Clinica. Clinica Universidad Navarra (CUN)|