Oral Bioavailability of Bilastine

NCT01124123 | Completed Phase 1

• 2 other identifiers: BILA 2909/BA2010-019049-25
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy

Keywords

Pharmacokinetics; Oral bioavailability; absorption; AUC; Bioequivalence; Bioavailability study

Outcome Measures

Primary Outcomes (1)

• The area under the plasma concentration versus time curve from time zero to infinity (AUC 0-∞ ).

  Bilastine bioavailability will be obtained from the oral AUC 0-∞ / endovenous AUC 0-∞ quotient.

  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.

Secondary Outcomes (2)

• Additional pharmacokinetic variables: Cmax, AUC 0-t, tmax, Ae, CLr and t ½

  17 blood draws and urine collection during 72 hours post administration

• Safety and tolerability of a single dose administration of oral and endovenous bilastine

  A last Follow up visit will be performed 7 days after last drug intake

Study Arms (2)

Bilastine 20 mg

EXPERIMENTAL

Single dose 20 mg bilastine oral tablet. Test drug

Drug: Bilastine

Bilastine 10 mg

ACTIVE COMPARATOR

Single dose 10 mg Bilastine endovenous. Control drug

Drug: Bilastine

Interventions

Bilastine DRUG

20 mg oral tablet

Bilastine 20 mg

Eligibility Criteria

• Age: 18 Years - 35 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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.
• Donation or loss of greater than 200 mL of blood within 12 weeks before entry to the study.
• 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.

Sponsors & Collaborators

• Faes Farma, S.A.: lead

Study Sites (1)

Unidad de Investigacion Clinica. Clinica Universidad de Navarra

Pamplona, Navarre, 31008, Spain

Location

Related Publications (3)

• Jauregizar N, de la Fuente L, Lucero ML, Sologuren A, Leal N, Rodriguez M. Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet. 2009;48(8):543-54. doi: 10.2165/11317180-000000000-00000.

  PMID: 19705924 BACKGROUND

• Lucero ML, Gonzalo A, Ganza A, Leal N, Soengas I, Ioja E, Gedey S, Jahic M, Bednarczyk D. Interactions of bilastine, a new oral H(1) antihistamine, with human transporter systems. Drug Chem Toxicol. 2012 Jun;35 Suppl 1:8-17. doi: 10.3109/01480545.2012.682653.

  PMID: 22616811 BACKGROUND

• Sadaba B, Gomez-Guiu A, Azanza JR, Ortega I, Valiente R. Oral availability of bilastine. Clin Drug Investig. 2013 May;33(5):375-81. doi: 10.1007/s40261-013-0076-y.

  PMID: 23529786 DERIVED

Related Links

• Clinical Trials and Medical Research page. Clinica Universidad Navarra (CUN)
• Clinical Pharmacology Department. Clinica Universidad Navarra (CUN)

MeSH Terms

Interventions

bilastine

Study Officials

• Belen Sadaba, MD

  Unidad de Investigacion Clinica. Clinica Universidad Navarra (CUN)

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 13, 2010
• First Posted: May 14, 2010
• Study Start: May 1, 2010
• Primary Completion: June 1, 2010
• Study Completion: September 1, 2010
• Last Updated: September 26, 2012

Record last verified: 2012-09

Locations

ES (1)