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Bioequivalence Study Between Levocetirizine Oral Disintegrating Tablet (ODT) and Levocetirizine Immediate Release Tablet (IRT)

Primary Purpose

Rhinitis

Status

Completed

Phase

Phase 1

Locations

Japan

Study Type

Interventional

Intervention

Levocetirizine IRT 5 mg

Levocetirizine ODT 5 mg

About this trial

This is an interventional treatment trial for Rhinitis focused on measuring Oral disintegrating tablet, Levocetirizine, Immediate release tablet, Bioequivalence, Japanese subjects

Eligibility Criteria

20 Years - 55 Years (Adult)MaleAccepts Healthy Volunteers

Inclusion Criteria:

Subjects must be 20 to 55 years of age inclusive, at the time of signing the informed consent.
Japanese subjects who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring.
Subjects with body weight of >= 50 kilogram (kg) and body mass index (BMI) within the range of >=18.5 and <25.0 kg per meter square (m^2).
In male subjects contraceptive use should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies.
Male subjects are eligible to participate if they agree to the following during the intervention period and until the completion of follow-ups: Refrain from donating sperm; Be abstinent from heterosexual or homosexual intercourse as their preferred and usual lifestyle (abstinent on a long term and persistent basis) and agree to remain abstinent; Agree to use a male condom and female partner to use an additional highly effective contraceptive method with a failure rate of <1 percentage per year when having sexual intercourse with a woman of childbearing potential who is not currently pregnant; Agree to use male condom when engaging in any activity that allows for passage of ejaculate to another person.
Subjects must be non-smokers.
Subjects capable of giving signed informed consent.

Exclusion Criteria:

Subjects with history or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; constituting a risk when taking the study intervention; or interfering with the interpretation of data.
Subjects with abnormal blood pressure as determined by the investigator.
Subjects with history of allergic rhinitis.
Subjects with ALT >1.5x upper limit of normal (ULN).
Subjects with bilirubin >1.5 times ULN (isolated bilirubin >1.5 times ULN is acceptable if bilirubin is fractionated and direct bilirubin <35 percentage).
Subjects with current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
Subjects with QTc >450 millisecond (msec).
Subjects with past or intended use of over-the-counter or prescription medication including vitamins, diet supplements (including St. John's wort), herbal medications within 14 days prior to first dosing or 5 half-lives (whichever is longer).
Exposure to more than 4 new chemical entities within 12 months prior to the first dosing day.
Current enrolment or past participation within 4 months prior to the first dosing day in this or any other clinical study involving an investigational study intervention or any other type of medical research (except for the subjects with no study intervention administered during any of those enrolment or participation).
The subject with positive serological test for syphilis (Rapid Plasma Reagin [RPR] and Treponema pallidum [TP] antibody tests), Human immunodeficiency virus (HIV) Antigen/Antibody, Hepatitis B surface antigen (HBsAg), Hepatitis C virus (HCV) antibody, or Human T-cell lymphotropic virus type 1 (HTLV-1) antibody at screening.
Subject with positive pre-study drug screen.
Subject with regular moderate alcohol consumption within 6 months prior to the study participation defined as: An average weekly intake of >14 units for males. One unit is equivalent to 360 milliliter (mL) of beer, 150 mL of wine or 45 mL of 80 proof distilled of spirits.
Smoking or history or regular use of tobacco- or nicotine-containing products within 6 months prior to screening.
Sensitivity to any of the study interventions, or components thereof, or drug or other allergy that, in the opinion of the investigator or Medical Monitor, contraindicates participation in the study.
History of donation of blood or blood products >= 400 mL within 3 months or >=200 mL within 1 month prior to the first dosing day.

Sites / Locations

GSK Investigational Site

Arms of the Study

Arm 1

Arm 2

Arm 3

Arm 4

Arm Type

Experimental

Arm Label

Subjects of Group A: Part 1

Subjects of Group B: Part 1

Subjects of Group C: Part 2

Subjects of Group D: Part 2

Arm Description

Subjects in Group A will be randomized to receive levocetirizine IRT 5 mg with 150 mL water in fasted state in Period 1. After a washout period of at least 5 days, subjects will receive levocetirizine ODT 5 mg with 150 mL water in fasted state in Period 2.

Subjects in Group B will be randomized to receive levocetirizine ODT 5 mg with 150 mL water in fasted state in Period 1. After a washout period of at least 5 days, subjects will receive levocetirizine IRT 5 mg with 150 mL water in fasted state in Period 2.

Subjects in Group C will be randomized to receive levocetirizine IRT 5 mg with 150 mL water in fasted state in Period 1. After a washout period of at least 5 days, subjects will receive levocetirizine ODT 5 mg without water in fasted state in Period 2.

Subjects in Group D will be randomized to receive levocetirizine ODT 5 mg without water in fasted state in Period 1. After a washout period of at least 5 days, subjects will receive levocetirizine IRT 5 mg with 150 mL water in fasted state in Period 2.

Outcomes

Primary Outcome Measures

Part 1: Area Under the Concentration-time Curve (AUC) From Time Zero Time (Pre-dose) to the Time of Last Quantifiable Concentration (AUC[0-t]) of Levocetirizine

Blood samples were collected to measure AUC(0-t) at indicated time-points. AUC(0-t) was calculated by the linear trapezoidal method (i.e., Linear Trapezoidal Linear Interpolation calculation method in Phoenix WinNonlin).

Part 2: AUC(0-t) of Levocetirizine

Part 1: Maximum Observed Concentration (Cmax) of Levocetirizine

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data.

Part 2: Cmax of Levocetirizine

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data.

Secondary Outcome Measures

Part 1: Area Under the Concentration-time Curve From Zero Time (Pre-dose) Extrapolated to Infinite Time AUC(0-inf) of Levocetirizine

Blood samples were collected at indicated time points for analysis of AUC(0-inf). AUC(0-inf)) of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: AUC(0-inf) of Levocetirizine

Blood samples were collected at indicated time points for analysis of AUC(0-inf). AUC(0-inf) of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 1: Time to First Occurrence of Cmax (Tmax) of Levocetirizine

Blood samples were collected at indicated time points for analysis of tmax. The tmax of levocetirizine was obtained directly from the concentration-time data. The tmax was analyzed with the non-parametric Wilcoxon Matched Pairs Method (Signed Rank Method) to compute point estimate and associated 90% confidence interval for the median difference.

Part 2: Tmax of Levocetirizine

Part 1: Apparent Terminal Phase Half-life (t1/2) of Levocetirizine

Blood samples were collected at indicated time points for analysis of t1/2. The t1/2 of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: t1/2 of Levocetirizine

Part 1: Percentage of AUC(0-inf) Obtained by Extrapolation (%AUCex) of Levocetirizine

Blood samples were collected at indicated time points for analysis of %AUCex. Percentage AUCex of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: %AUCex of Levocetirizine

Part 1: Apparent Clearance Following Oral Dosing (CL/F) of Levocetirizine

Blood samples were collected at indicated time points for analysis of CL/F. CL/F of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: CL/F of Levocetirizine

Part 1: Apparent Volume of Distribution Following Oral Dosing (Vz/F) of Levocetirizine

Blood samples were collected at indicated time points for analysis of Vz/F. Vz/F of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: Vz/F of Levocetirizine

Blood samples were collected at indicated time points for analysis of Vz/F. Vz/F of levocetirizine was calculated as by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 1: Elimination Rate Constant (Kel) (lambda_z) of Levocetirizine

Blood samples were collected at indicated time points for analysis of kel. kel (lambda_z) is the first order rate constant associated with the terminal (log-linear) portion of the curve. kel of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: Kel (lambda_z) of Levocetirizine

Part 1: Mean Residence Time (MRT) of Levocetirizine

Blood samples were collected at indicated time points for analysis of MRT. MRT of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher).

Part 2: MRT of Levocetirizine

Part 1: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. A SAE is defined as any untoward medical occurrence that, at any dose may results in death or is life-threatening or requires inpatient hospitalization or results in persistent disability/incapacity or is a congenital anomaly/birth defect or any other situation according to medical or scientific judgment.

Part 2: Number of Participants With AEs and SAEs

Part 1: Change From Baseline in Albumin and Total Protein Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in albumin and total protein levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Albumin and Total Protein Levels

Part 1: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in alkaline phosphatase, alanine amino transferase, aspartate amino transferase, creatine kinase, gamma glutamyl transferase and lactate dehydrogenase levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels

Part 1: Change From Baseline in Amylase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Amylase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in amylase levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 1: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in direct bilirubin, total bilirubin, creatinine and uric acid levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels

Part 1: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/Blood Urea Nitrogen (BUN) Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in calcium, cholesterol, chloride, glucose, high density lipids cholesterol, potassium, low density lipids cholesterol, sodium, phosphorus inorganic, triglycerides and urea/blood urea nitrogen (BUN) levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/BUN Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in calcium, cholesterol, chloride, glucose, high density lipids cholesterol, potassium, low density lipids cholesterol, sodium, phosphorus inorganic, triglycerides and urea/BUN levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 1: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in basophils, eosinophils, lymphocytes, monocytes and total neutrophils levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count

Part 1: Change From Baseline in Platelet Count and White Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in platelet count and white blood cell count were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Platelet Count and White Blood Cell Count

Part 1: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hemoglobin and mean corpuscle hemoglobin concentration were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration

Part 1: Change Form Baseline in Hematocrit

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hematocrit was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change Form Baseline in Hematocrit

Part 1: Change From Baseline in Mean Corpuscle Hemoglobin

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle hemoglobin was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Mean Corpuscle Hemoglobin

Part 1: Change From Baseline in Mean Corpuscle Volume

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle volume was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Mean Corpuscle Volume

Part 1: Change From Baseline in Red Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in red blood cell count was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Red Blood Cell Count

Part 1: Change From Baseline in Reticulocytes

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in reticulocytes was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Reticulocytes

Part 1: Number of Participants With Urinalysis Results by Dipstick Method

Urine samples were collected to assess urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen by dipstick test. The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen can be read as negative (-), trace and 1+ indicating proportional concentrations in the urine sample. Only categories with significant values have been presented.

Part 2: Number of Participants With Urinalysis Results by Dipstick Method

Part 1: Urine Potential of Hydrogen (pH)

Urine samples were collected for the measurement of urine pH. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acid pH (5.0 - 6.0).

Part 2: Urine Potential of Hydrogen (pH)

Part 1: Urine Specific Gravity

Urine samples were collected for the measurement of specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. The concentration of the excreted molecules determines the urine's specific gravity. The urinary specific gravity measurement is a routine part of urinalysis. The reference range is 1.002-1.030.

Part 2: Urine Specific Gravity

Part 1: Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Blood pressure was measured in supine position after 5 minutes rest. Change from Baseline in SBP and DBP was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in SBP and DBP

Part 1: Change From Baseline in Heart Rate

Heart rate was measured in supine position after 5 minutes rest. Change from Baseline in heart rate was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Heart Rate

Part 1: Change From Baseline in Body Temperature

Body temperature was measured in supine position after 5 minutes rest. Change from Baseline in body temperature was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Body Temperature

Part 1: Change From Baseline in Heart Rate (12-Lead Electrocardiogram [ECG])

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QT interval with Fridericia's correction (QTcF). Change from Baseline in heart rate (ECG) was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in Heart Rate (ECG)

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in heart rate (ECG) was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 1: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in PR interval, QRS interval, QT interval and QTcF interval was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value.

Part 2: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in PR interval, QRS interval, QT interval and QTcF interval was evaluated. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits.

Full Information

NCT ID

NCT03555890

First Posted

May 9, 2018

Last Updated

May 22, 2020

Sponsor

GlaxoSmithKline

Collaborators

Zensei Pharmaceutical Co., Ltd.

1. Study Identification

Unique Protocol Identification Number

NCT03555890

Brief Title

Bioequivalence Study Between Levocetirizine Oral Disintegrating Tablet (ODT) and Levocetirizine Immediate Release Tablet (IRT)

Official Title

A Single Centre, Single Dose, Open-label, Randomized, 2-part, 2-way Crossover Study to Determine the Bioequivalence of Levocetirizine Oral Disintegrating Tablet Given With Water and Without Water Compared to Levocetirizine Immediate Release Tablet in Healthy Japanese Male Subjects

Study Type

Interventional

2. Study Status

Record Verification Date

May 2020

Overall Recruitment Status

Completed

Study Start Date

May 18, 2018 (Actual)

Primary Completion Date

September 17, 2018 (Actual)

Study Completion Date

September 17, 2018 (Actual)

3. Sponsor/Collaborators

Responsible Party, by Official Title

Sponsor

Name of the Sponsor

GlaxoSmithKline

Collaborators

Zensei Pharmaceutical Co., Ltd.

4. Oversight

Studies a U.S. FDA-regulated Drug Product

Studies a U.S. FDA-regulated Device Product

Data Monitoring Committee

5. Study Description

Brief Summary

This study will be an open-label, randomized 2-way cross-over study to evaluate bioequivalence study between levocetirizine ODT and levocetirizine IRT in healthy Japanese male subjects. Approximately 48 subjects will participate in this study to receive a single dose treatments of levocetirizine ODT 5 milligram (mg) or levocetirizine IRT 5 mg. In Part 1, subjects will randomized in 1:1 ratio (12 in each Period) in Period 1 and 2 to receive single dose of levocetirizine ODT 5 mg with water or single dose levocetirizine IRT 5 mg with water in fasted state. In this part, comparison of bioavailability of levocetirizine ODT and levocetirizine IRT when taken with water in the fasted state will be assessed. In Part 2, subjects will be randomized in 1:1 ratio (12 in each Period) in Period 1 and 2 to receive single dose levocetirizine ODT 5 mg without water or single dose levocetirizine IRT 5 mg with water in fasted state. In this part, comparison of bioavailability of levocetirizine ODT without water and levocetirizine IRT with water in the fasted state will be assessed. There will be at least a 5-day wash out period between the intervention periods. The duration of each subject's participation in each part will be approximately 7 weeks from screening to follow-up.

6. Conditions and Keywords

Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study

Rhinitis

Keywords

Oral disintegrating tablet, Levocetirizine, Immediate release tablet, Bioequivalence, Japanese subjects

7. Study Design

Primary Purpose

Treatment

Study Phase

Phase 1

Interventional Study Model

Crossover Assignment

Model Description

This study is 2-way crossover 2 part study. In Part 1, comparison of bioavailability of levocetirizine ODT and levocetirizine IRT taken with water in the fasted state will be done and In Part 2, comparison of bioavailability of levocetirizine ODT without water and levocetirizine IRT with water in the fasted state will be done.

Masking

None (Open Label)

Allocation

Randomized

Enrollment

72 (Actual)

8. Arms, Groups, and Interventions

Arm Title

Subjects of Group A: Part 1

Arm Type

Experimental

Arm Description

Arm Title

Subjects of Group B: Part 1

Arm Type

Experimental

Arm Description

Arm Title

Subjects of Group C: Part 2

Arm Type

Experimental

Arm Description

Arm Title

Subjects of Group D: Part 2

Arm Type

Experimental

Arm Description

Intervention Type

Drug

Intervention Name(s)

Levocetirizine IRT 5 mg

Intervention Description

Levocetirizine IRT will be available as film-coated tablets. Subjects will receive a single dose of 5 mg levocetirizine IRT. Subjects will receive levocetirizine IRT with 150 mL water in both Part (1 and 2).

Intervention Type

Drug

Intervention Name(s)

Levocetirizine ODT 5 mg

Intervention Description

Levocetirizine ODT will be available as oral disintegrating tablet. Subjects will receive a single dose of 5 mg levocetirizine ODT. In Part 1, subjects will receive levocetirizine ODT with 150 mL water and in Part 2 subjects will receive levocetirizine ODT without water.

Primary Outcome Measure Information:

Title

Part 1: Area Under the Concentration-time Curve (AUC) From Time Zero Time (Pre-dose) to the Time of Last Quantifiable Concentration (AUC[0-t]) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

Title

Part 2: AUC(0-t) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

Title

Part 1: Maximum Observed Concentration (Cmax) of Levocetirizine

Description

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data.

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

Title

Part 2: Cmax of Levocetirizine

Description

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data.

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

Secondary Outcome Measure Information:

Title

Part 1: Area Under the Concentration-time Curve From Zero Time (Pre-dose) Extrapolated to Infinite Time AUC(0-inf) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: AUC(0-inf) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Time to First Occurrence of Cmax (Tmax) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: Tmax of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Apparent Terminal Phase Half-life (t1/2) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: t1/2 of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Percentage of AUC(0-inf) Obtained by Extrapolation (%AUCex) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: %AUCex of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Apparent Clearance Following Oral Dosing (CL/F) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: CL/F of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Apparent Volume of Distribution Following Oral Dosing (Vz/F) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: Vz/F of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Elimination Rate Constant (Kel) (lambda_z) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: Kel (lambda_z) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Mean Residence Time (MRT) of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 2: MRT of Levocetirizine

Description

Time Frame

Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

Title

Part 1: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Description

Time Frame

Up to 18 days

Title

Part 2: Number of Participants With AEs and SAEs

Description

Time Frame

Up to 18 days

Title

Part 1: Change From Baseline in Albumin and Total Protein Levels

Description

Time Frame