Cetirizine Chewable Bioequivalence and Food Effect Study

NCT03772158 | Completed Phase 1 FDA Drug

• 1 other identifier: CCSURA000499
• Study Type: interventional
• Target: 40
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to determine and compare the amount of study drug that gets into your blood after the administration of each of the three formulations of cetirizine under different conditions. Another objective of this study is to evaluate the effect of food on the amount of study drug that gets into your blood after the administration of the investigational formulation. Other objectives of this study are to determine the sensory experience and ease of swallowing the investigational formulation, as well as to determine the safety of test and reference formulations of cetirizine.

Conditions

Allergy

Keywords

Bioequivalence study; Healthy volunteers; Cetirizine; Tablet

Outcome Measures

Primary Outcomes (2)

• The maximum observed plasma concentration (Cmax) of cetirizine

  The maximum observed plasma concentration.

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

• The area under the plasma concentration versus time curves to the last measurable concentration (AUCt)

  Area under the plasma concentration versus time curve from start of drug administration until last measurable concentration.

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

Secondary Outcomes (7)

• Area under the plasma concentration versus time curve extrapolated to infinity

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

• The time point at which the maximum concentration of cetirizine is observed (Tmax).

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

• The terminal elimination half-life (T1/2) of cetirizine in plasma

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

• The terminal elimination rate constant (lambda z) for cetirizine in plasma.

  At baseline, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 12, 24, 28 and 32 hours after the start of dose administration.

• To assess subject's sensory experience and ease of swallowing of the test product

  Assessed one minute after dosing, and preferably completed within 15 minutes of dosing for treatments A, B and C

Study Arms (5)

Treatment A

EXPERIMENTAL

Single dose of 10 mg cetirizine as a chewable tablet, administered orally after a 10-hour overnight fast and followed with 240 mL ambient water. Subjects will be instructed to chew the tablet completely before swallowing.

Drug: Cetirizine 10mg

Treatment B

EXPERIMENTAL

Single dose of 10 mg cetirizine as a chewable tablet, administered orally after a 10-hour overnight fast without water. Subjects will be instructed to chew the tablet completely before swallowing.

Drug: Cetirizine 10mg

Treatment C

EXPERIMENTAL

Single dose of 10 mg cetirizine as a chewable tablet, administered orally after a 10-hour overnight fast and 30 minutes after the start of the standard high-fat breakfast and followed with 240 mL ambient water. Subjects will be instructed to chew the tablet completely before swallowing.

Drug: Cetirizine 10mg

Treatment D

ACTIVE COMPARATOR

Single dose of currently marketed US 10 mg cetirizine as immediate release tablet (ZYRTEC®), administered orally after a 10-hour overnight fast and followed with 240 mL ambient water.

Drug: Cetirizine 10 mg

Treatment E

ACTIVE COMPARATOR

Single dose of currently marketed EU/Australian 10 mg cetirizine film coated tablet (REACTINE®) administered orally after a 10-hour overnight fast and followed with 240 mL ambient water.

Drug: Cetirizine 10 mg

Interventions

Cetirizine 10mg DRUG

Chewable tablet

Also known as: Test product

Treatment A; Treatment B; Treatment C

Cetirizine 10 mg DRUG

Immediate Release Tablet

Also known as: ZYRTEC 10 mg

Treatment D

Eligibility Criteria

• Age: 18 Years - 55 Years
• Gender Eligibility Details: No less than approximately 40% of either gender will be represented in the study population.
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male or female subject between the ages of 18 and 55 years, inclusive. Health is defined as the absence of clinically relevant abnormalities as judged by the Investigator on the basis of a detailed medical history, physical examination, blood pressure, pulse rate measurements, 12-lead electrocardiogram (ECG), as well as clinical laboratory tests. The responsible Investigator may request additional investigations or analyses if necessary.
• Non- or ex-tobacco user, being defined as someone who completely stopped smoking or using any form of tobacco or nicotine-containing product for at least 6 months before screening visit of this study.
• For females: Postmenopausal state (i.e. at least 1 year without menses without an alternative medical condition prior to the first study drug administration) or premenopausal /perimenopausal state with an effective means of contraception (as defined in Section 10.5.5).
• For males: No pregnant or lactating spouse or partner at screening and willingness to utilize an acceptable form of birth control with spouse or any potential partner during the study.
• Body Mass Index (BMI) ≥ 18.5 and ≤ 30 kg/m2 with a total body weight \>50 kg.
• A personally signed and dated informed consent document, indicating that the subject has been informed of all pertinent aspects of the study.
• Is able to comprehend the requirements of the study (based upon clinical site personnel's assessment) and is willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures specified within the protocol.

You may not qualify if:

• Use of prescription or non-prescription medications within 5 half-lives before the first IP administration unless these are contraceptives or occasional use of other medications approved by the Investigator.
• Use of any vitamins, dietary and herbal supplements within seven days before first dose of study drug.
• History of any allergy or hypersensitivity (e.g. skin reaction, asthma, angioedema) to cetirizine or any excipients of the formulations.
• If female: is pregnant, has a positive pregnancy test at screening or prior to the first study drug administration, or is planning to become pregnant during the duration of the study, and/or is breast-feeding.
• Has a history of gastrointestinal surgery other than appendectomy.
• Has hypertension, fluid retention, or heart disease either by history or by the medically qualified Investigator's medical judgment.
• Currently suffering from asthma or has a medically significant history of asthma in the opinion of the investigator.
• Has clinically significant renal or hepatic impairment; according to the medically qualified Investigator discretion.
• Was treated with an investigational product within 28 days or within a period less than 5 times the drug's half-life, whichever is longer, preceding the first dose of study drug.
• Preplanned surgical procedures during the study period as this may interfere with the conduct of the study.
• History of alcoholism or substance abuse, as judged by the Investigator, within the past 6 months preceding this study.
• Consumed alcohol beverage(s) within 48 hours preceding the first dose of study drug.
• History of rare hereditary problems of galactose and/or lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
• Any history of tuberculosis.
• Donation or loss of blood within 28 days prior to the first treatment visit if the estimated lost blood volume equaled or exceeded 50 mL.

Sponsors & Collaborators

• Johnson & Johnson Consumer Inc., McNeil Consumer Healthcare Division: lead

Study Sites (1)

Algorithme (An altascience Company)

Mount Royal, Quebec, H3P 3P1, Canada

Location

Related Links

• CSR synopsis for Bioequivalence Study.

MeSH Terms

Conditions

Hypersensitivity

Interventions

Cetirizine

Condition Hierarchy (Ancestors)

Immune System Diseases

Intervention Hierarchy (Ancestors)

Hydroxyzine; Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Eric Sicard, MD

  Algorithme Pharma Inc

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Who Masked: OUTCOMES ASSESSOR
• Masking Details: Blinding of the test and reference products to study subjects is not feasible, because the products are different dosage forms (chewable tablets and IR tablets) and administered in different ways (with or without water and fasted or fed). Personnel conducting the bioanalyses of samples will not know the treatment sequence. The randomization code will not be available to them until the analytical tables have been finalized and audited by the Algorithme Pharma (An Altasciences Company) Quality Assurance (QA) department.
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: This is a randomized, single-dose, four-treatment crossover bioequivalence and food effect study of Cetirizine Chewable Tablets versus ZYRTEC® Immediate Release (IR) Tablets (US reference) and REACTINE® IR Tablets (EU and Australian marketed reference product). The study will be conducted in two parts. Part 1 of the study will have a randomized, four way crossover study design in which 40 healthy subjects, ages 18 to 55 years, will be randomized to four sequences of Treatments A, B, D and E over consecutive periods. No less than approximately 40% of either gender will be represented in the study population. Part 2 of the study will assess a potential food effect in which all subjects will be administered Treatment C in the fifth period.

Study Record Dates

• First Submitted: December 10, 2018
• First Posted: December 11, 2018
• Study Start: December 11, 2018
• Primary Completion: February 3, 2019
• Study Completion: February 3, 2019
• Last Updated: December 1, 2021

Record last verified: 2021-11

Locations

CA (1)