To Assess Bioequivalence of Loratadine Oral Solution/Syrup Versus Claritin Peach Syrup (Bordeaux)

A Single-dose, Single-center, Randomized, Open-label, Two-way Crossover Study in Healthy Adults to Assess the Bioequivalence of Loratadine Oral Solution/Syrup 1mg/mL (GPLA Formula) Versus Claritin Peach Syrup 1mg/mL (ANNA Formula)

To assess the bioequivalence of Loratadine Oral Solution/Syrup 1mg/mL (GPLA Formula) versus Claritin Peach Syrup 1mg/mL (ANNA Formula)

Study Overview

• Status: Completed
• Conditions: Histamine H1 Antagonists, Non-Sedating
• Intervention / Treatment: Drug: Loratadine oral solution; Drug: Loratadine (Claritin peach syrup)

• Study Type: Interventional
• Enrollment (Actual): 54
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Bayern
    • Neu-Ulm, Bayern, Germany, 89231

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy adult (men or women), age 18 to 55 years inclusive;
• Body mass index 18.5 to 30.0 kg/m*2 inclusive;
• Able to read and understand the written informed consent for study-related information and instruction;
• Able to comply with protocol requirements, including overnight stays, blood sample collections as defined in the protocol;
• Agree not to donate whole blood or components of blood (e.g. plasma, thrombocytes) starting from signing the informed consent form through 30 days after the last study procedure, except for the blood samples collected for this study;
• Female subjects of childbearing potential must be using a medically acceptable form of birth control for at least 1 month prior to screening (3 months on oral contraceptives), e.g., oral or patch contraceptives, intrauterine device, injectable contraceptive (e.g. Depo-Provera), or a double barrier and have a negative pregnancy test at Screening and prior to study drug administration on Day 0 of Dosing Periods 1 and 2. Female subjects of non-childbearing potential must be amenorrheic for at least two years or had a hysterectomy and/or bilateral oophorectomy;

Exclusion Criteria:

• Pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal;
• Known hypersensitivity to any medication (active substances or excipients of the preparations) to be used in the study;
• Known galactose intolerance, lactase deficiency or glucose-galactose malabsorption
• Known severe allergies (e.g. allergies to more than 3 allergens, allergies affecting the lower respiratory tract - allergic asthma, allergies requiring therapy with corticosteroids);

• Use of, within 1 month before the first study drug administration, systemic or topical medicines or substances which might affect the study objectives, e.g

  • any drug known to induce cytochrome P3A4/5 or P Glycoprotein (e.g. rifampin, carbamazepine, St. John's wort);
  • any drug known to inhibit cytochrome P3A4/5 or P Glycoprotein (e.g. erythromycin, clarithromycin, chloramphenicol, ketoconazole);
  • any drug known to induce cytochrome P2D6 (e.g. rifampin, dexamethasone);
  • any drug known to inhibit cytochrome P2D6 (e.g. cimetidine, desipramine, fluoxetine, metoclopramide);
• Positive urine pregnancy, urine drug test or Hepatitis B, hepatitis C or HIV tests;
• Clinically relevant findings in the physical examination, e.g., signs of bleeding diathesis, signs of heart failure, evidence of peripheral circulatory disturbances, and skin abnormalities;

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Loratadine oral solution/syrup then Claritin peach syrup; Subjects received a single oral dose of 10 mg loratadine-oral solution/syrup 1 mg/mL (GPLA formula, test formulation) under fasted condition in treatment period 1, followed by a single oral dose of 10 mg loratadine-claritin peach syrup 1 mg/mL (ANNA formula, reference formulation) under fasted condition in treatment period 2. A wash-out period of at least 10 calendar days was maintained between the 2 treatments.	Drug: Loratadine oral solution; Subjects received a single oral dose of 10 mg loratadine oral solution/syrup 1 mg/mL (GPLA formula, test formulation) under fasted condition in any intervention period.; Drug: Loratadine (Claritin peach syrup); Subjects received a single oral dose of 10 mg loratadine claritin peach syrup 1 mg/mL (ANNA formula, reference formulation) under fasted condition in any intervention period.
Experimental: Claritin peach syrup then Loratadine oral solution/syrup; Subjects received a single oral dose of 10 mg loratadine-claritin peach syrup 1 mg/mL (ANNA formula, reference formulation) under fasted condition in treatment period 1, followed by a single oral dose of 10 mg loratadine-oral solution/syrup 1 mg/mL (GPLA formula, test formulation) under fasted condition in treatment period 2. A wash-out period of at least 10 calendar days was maintained between the 2 treatments.	Drug: Loratadine oral solution; Subjects received a single oral dose of 10 mg loratadine oral solution/syrup 1 mg/mL (GPLA formula, test formulation) under fasted condition in any intervention period.; Drug: Loratadine (Claritin peach syrup); Subjects received a single oral dose of 10 mg loratadine claritin peach syrup 1 mg/mL (ANNA formula, reference formulation) under fasted condition in any intervention period.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Primary: Area Under the Concentration Versus Time Curve From Zero to the Last Data Point Greater Than Lower Limit of Quantitation (LLOQ) of Loratadine in Plasma (AUC[0-tlast]) After Single Oral Dose of Loratadine	Area under the concentration versus time curve from zero to the last data point greater than (>) LLOQ (AUC[0-tlast]) after single dose.	0 hour (h) (pre-dose) to 72 h post-dose
Maximum Observed Concentration (Cmax) of Loratadine in Plasma After Single Oral Dose of Loratadine	Maximum observed loratadine concentration in plasma, directly taken from analytical data.	0 h (pre-dose) to 72 h post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Time to Reach Maximum Concentration (tmax) in Plasma After Single Dose of Loratadine	Time to reach maximum loratadine concentration in plasma after its single oral dose, directly taken from analytical data.	0 h (pre-dose) to 72 h post-dose
Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC) of Loratadine in Plasma After Single Dose	Area under the concentration versus time curve from zero to infinity after single dose.	0 h (pre-dose) to 72 h post-dose
Half-Life (t1/2) Associated With the Terminal Slope of Loratadine After Single Dose	Half-life associated with the terminal slope.	0 h (pre-dose) to 72 h post-dose
Total Body Clearance (CL/F) of Loratadine Calculated After its Single Oral Administration	Total body clearance of loratadine calculated after extravascular application.	0 h (pre-dose) to 72 h post-dose
Percentage of Area Under the Concentration Versus Time Curve (AUC) From the Last Calculated Data Point Greater Than Lower Limit of Quantification [LLOQ]) to Infinity (%AUC[tlast-∞]) After Single Oral Administration of Loratadine	Percentage of AUC from the last calculated data point > LLOQ to infinity was measured.	0 h (pre-dose) to 72 h post-dose
Apparent Terminal Rate Constant (λz) of Loratadine After Single Dose	Apparent terminal rate constant, calculated from the slope of a log-linear regression of the unweighted data considering the last concentration-time points > LLOQ.	0 h (pre-dose) to 72 h post-dose
Area Under the Concentration Versus Time Curve From Zero to 72 Hours (AUC[0-72]) of Lloratadine in Plasma After Single Oral Dose	Area under the concentration versus time curve from zero to 72 h after single dose.	0 h (pre-dose) to 72 h post-dose
Maximum Observed Concentration (Cmax) of Desloratadine in Plasma After Single Oral Dose of Loratadine	Maximum observed desloratadine concentration in plasma, directly taken from analytical data.	0 h (pre-dose) to 72 h post-dose
Time to Reach Maximum Concentration (tmax) of Desloratadine in Plasma After Single Dose of Loratadine	Time to reach maximum drug concentration in the measured matrix, directly observed from the analytical data.	0 h (pre-dose) to 72 h post-dose
Area Under the Concentration Versus Time Curve From Zero to the Last Data Point Greater Than Lower Limit of Quantitation (LLOQ) of Desoratadine in Plasma (AUC[0-tlast]) After Single Oral Dose of Loratadine	Area under the concentration versus time curve from zero to the last data point > LLOQ (AUC[0-tlast]) after single dose.	0 h (pre-dose) to 72 h post-dose
Area Under the Concentration Versus Time Curve From Zero to 72 Hours (AUC[0-72]) of Desloratadine in Plasma After Single Oral Dose of Loratadine	Area under the concentration versus time curve from zero to 72 h after single dose. AUC and residual area were not evaluated because the concentration at 72 h was quantifiable in the majority of profiles.	0 h (pre-dose) to 72 h post-dose
Time of Last Concentration Above the Lower Limit Of Quantitation (LLOQ) of Desloratadine, Directly Taken From Analytical Data (tlast)	Time of last concentration above LLOQ, directly taken from analytical data.	0 h (pre-dose) to 72 h post-dose
Half-Life (t1/2) Associated With the Terminal Slope of Desoratadine After Single Dose of Loratadine	Half-life associated with the terminal slope.	0 h (pre-dose) to 72 h post-dose
Percentage of Area Under the Concentration Versus Time Curve (AUC) from the Last Data Point Greater Than Lower Limit of Quantitation (LLOQ) to Infinity (%AUC[tlast-∞]) of Desoratadine After Single Oral Administration of Loratadine	Percentage of area under the concentration versus time curve from zero to the last data point > LLOQ in plasma (AUC[(0-tlast]) was measured.	0 h (pre-dose) to 72 h post-dose
Apparent Terminal Rate Constant (λz) of Desoratadine After Single Dose of Loratadine	Apparent terminal rate constant, calculated from the slope of a log-linear regression of the unweighted data considering the last concentration-time points > LLOQ.	0 h (pre-dose) to 72 h post-dose

Collaborators and Investigators

• Sponsor: Bayer

Publications and helpful links

Helpful Links

• Click here to find information about studies related to Bayer Healthcare products conducted in Europe

Study record dates

Study Major Dates

• Study Start: December 1, 2015
• Primary Completion (Actual): January 1, 2016
• Study Completion (Actual): March 1, 2016

Study Registration Dates

• First Submitted: October 30, 2015
• First Submitted That Met QC Criteria: October 30, 2015
• First Posted (Estimate): November 1, 2015

Study Record Updates

• Last Update Posted (Actual): February 13, 2017
• Last Update Submitted That Met QC Criteria: February 10, 2017
• Last Verified: February 1, 2017

More Information

Terms related to this study

• Keywords: Allergy
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Dermatologic Agents; Anti-Allergic Agents; Histamine H1 Antagonists; Histamine Antagonists; Histamine Agents; Antipruritics; Histamine H1 Antagonists, Non-Sedating; Loratadine
• Other Study ID Numbers: 18199; 2015-002720-12 (EudraCT Number)