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

Phase 1

Completed

• Conditions: Histamine H1 Antagonists, Non-Sedating
• Interventions: Drug: Loratadine oral solution; Drug: Loratadine (Claritin peach syrup)

• Registration Number: NCT02593747
• Lead Sponsor: Bayer

Brief Summary

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

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2015-10-30
• Study First Submitted QC: 2015-10-30
• Study First Posted: 2015-11-01
• Study Start: 2015-12
• Primary Completion: 2016-01
• Study Completion: 2016-03
• Status Verified: 2017-02
• Last Update Submitted: 2017-02-10
• Last Update Posted: 2017-02-13

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 54

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;

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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;

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Claritin peach syrup then Loratadine oral solution/syrup	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 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.
Loratadine oral solution/syrup then Claritin peach syrup	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 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.
Claritin peach syrup then Loratadine oral solution/syrup	Loratadine oral solution	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.
Loratadine oral solution/syrup then Claritin peach syrup	Loratadine (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.

Primary Outcome Measures

Name	Time	Method
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	0 hour (h) (pre-dose) to 72 h post-dose	Area under the concentration versus time curve from zero to the last data point greater than (\>) LLOQ (AUC\[0-tlast\]) after single dose.
Maximum Observed Concentration (Cmax) of Loratadine in Plasma After Single Oral Dose of Loratadine	0 h (pre-dose) to 72 h post-dose	Maximum observed loratadine concentration in plasma, directly taken from analytical data.

Secondary Outcome Measures

Name	Time	Method
Time to Reach Maximum Concentration (tmax) in Plasma After Single Dose of Loratadine	0 h (pre-dose) to 72 h post-dose	Time to reach maximum loratadine concentration in plasma after its single oral dose, directly taken from analytical data.
Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC) of Loratadine in Plasma After Single Dose	0 h (pre-dose) to 72 h post-dose	Area under the concentration versus time curve from zero to infinity after single dose.
Time to Reach Maximum Concentration (tmax) of Desloratadine in Plasma After Single Dose of Loratadine	0 h (pre-dose) to 72 h post-dose	Time to reach maximum drug concentration in the measured matrix, directly observed from the analytical data.
Half-Life (t1/2) Associated With the Terminal Slope of Loratadine After Single Dose	0 h (pre-dose) to 72 h post-dose	Half-life associated with the terminal slope.
Area Under the Concentration Versus Time Curve From Zero to 72 Hours (AUC[0-72]) of Lloratadine in Plasma After Single Oral Dose	0 h (pre-dose) to 72 h post-dose	Area under the concentration versus time curve from zero to 72 h after single dose.
Time of Last Concentration Above the Lower Limit Of Quantitation (LLOQ) of Desloratadine, Directly Taken From Analytical Data (tlast)	0 h (pre-dose) to 72 h post-dose	Time of last concentration above LLOQ, directly taken from analytical data.
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	0 h (pre-dose) to 72 h post-dose	Percentage of AUC from the last calculated data point \> LLOQ to infinity was measured.
Half-Life (t1/2) Associated With the Terminal Slope of Desoratadine After Single Dose of Loratadine	0 h (pre-dose) to 72 h post-dose	Half-life associated with the terminal slope.
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	0 h (pre-dose) to 72 h post-dose	Percentage of area under the concentration versus time curve from zero to the last data point \> LLOQ in plasma (AUC\[(0-tlast\]) was measured.
Total Body Clearance (CL/F) of Loratadine Calculated After its Single Oral Administration	0 h (pre-dose) to 72 h post-dose	Total body clearance of loratadine calculated after extravascular application.
Maximum Observed Concentration (Cmax) of Desloratadine in Plasma After Single Oral Dose of Loratadine	0 h (pre-dose) to 72 h post-dose	Maximum observed desloratadine concentration in plasma, directly taken from analytical data.
Apparent Terminal Rate Constant (λz) of Desoratadine After Single Dose of Loratadine	0 h (pre-dose) to 72 h post-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.
Apparent Terminal Rate Constant (λz) of Loratadine After Single Dose	0 h (pre-dose) to 72 h post-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.
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	0 h (pre-dose) to 72 h post-dose	Area under the concentration versus time curve from zero to the last data point \> LLOQ (AUC\[0-tlast\]) after single 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	0 h (pre-dose) to 72 h post-dose	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.