Clinical Pharmacology
Conditions
Keywords
Upper respiratory allergy symptoms including congestion
Brief summary
To evaluate the bioequivalence of one extended release combination (loratadine 5 mg/pseudoephedrine sulfate 120 mg) tablet manufactured for Bayer HealthCare LLC by SAG Manufacturing, S.L.U. Madrid, Spain (test treatment) to the extended release combination (loratadine 5 mg/pseudoephedrine sulfate 120 mg) tablet manufactured for Bayer SA-NV by Schering- Plough Labo NV Heist (reference treatment) which is currently marketed in Europe.
Interventions
Oral, Loratadine 5 mg/ pseudoephedrine sulfate 120 mg (x1)
Oral, Loratadine 5 mg/ pseudoephedrine sulfate 120 mg (x1)
Sponsors
Bayer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
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 * Be willing and able to consume all contents of the standardized breakfast within 30 minutes of dosing
Exclusion criteria
* Positive alcohol or drug screen at Screening or on Day -1 of each dosing period; * Use of within 1 month before first study drug administration, systemic or topical medicines or substances which might affect the study objectives, 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., clarithromycin, chloramphenicol, ketoconazole); * History of hypersensitivity symptoms with the use of loratadine, desloratadine (Clarinex), or pseudoephedrine; * Females who are pregnant or lactating * Known severe allergies (e.g., allergies to more than 3 allergens, allergies affecting the lower respiratory tract - allergic asthma, allergies requiring therapy with corticosteroids); * More than moderate alcohol consumption (\>40 g of alcohol regularly per day); * Any history or suspicion of barbiturate, amphetamine, benzodiazepine, cocaine, opiates, methamphetamine or cannabis abuse; * Loss of blood of 50 mL to 499 mL within 30 days of the first dose of trial treatment, or in excess of 500 mL within 56 days of the first dose of trial treatment (e.g., donation, plasmapheresis or injury)
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| AUC(0-tlast) of loratadine and pseudoephedrine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Area under the curve from time 0 to the last measurable concentration. |
| Cmax of loratadine and pseudoephedrine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Maximum observed plasma level |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Tmax for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Time at which Cmax is observed |
| Tlast for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Time point for last measurable concentration. |
| λz for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Terminal elimination rate constant |
| t1/2 for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Half-life |
| AUC for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Area under the curve from time 0 to infinity. |
| AUC(0-tlast) for desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Area under the curve from time 0 to the last measurable concentration. |
| Cmax for desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Maximum observed plasma level |
| Number of participants with adverse events | Up to 26 days | — |
| CL/F for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Total body oral clearance |
| %AUC(tlast-∞) for loratadine, pseudoephedrine and desloratadine | Baseline (within 60 minutes of dosing) and at 15, 30, 45, 60 minutes and 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 and 72 hours post dose in each treatment period | Percentage of AUC from last data point \> Lower limit of quantification (LLOQ) to infinity |
Countries
United States
Outcome results
None listed