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This study seeks to evaluate the comparative bioavailability of etoricoxib/betamethasone tablets 90 mg/0.25 mg test drug, administered in fixed combination vs. etoricoxib tablets 90 mg (Arcoxia®) reference drug, and betamethasone solution 50 mg/100 mL (Celestone® Pediatric) reference drug, administered individually, in a single dose, to 42 healthy mexican research subjects of both genders, under fasting conditions.
The purpose of this study is to determine whether there are differences in the magnitude and rate of absorption between the test drug and the reference drugs. The study will be cross-over, randomized, with three periods, three treatments, six sequences, truncated at 72 hours in 42 healthy subjetcs, with a single dose of etoricoxib/betamethasone 90/0.25 mg tablet administered in combination or a tablet of etoricoxib 90 mg, or betamethasone solution 50 mg/100 mL (Celestone® Pediatric) administered individually under fasting conditions, with 250 mL of water and a 14-day washout period between each dose of the test product.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Group A: Etoricoxib / Betamethasone | Experimental | Group A: Etoricoxib/ Betamethasone in fixed dose combination. Pharmaceutical form: Tablet. Each tablet contains:
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| Group B: Etoricoxib | Active Comparator | Group B: Etoricoxib Pharmaceutical form: Tablet. Formula: Each tablet contains 90 mg of Etoricoxib. Dosage: 1 tablet of 90 mg. Administration way: Oral. |
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| Group C: Betamethasone | Active Comparator | Group C: Betamethasone Pharmaceutical form: Solution. Formula: Each 100 mL of solution contains 50 mg of betamethasone. Dosage: 0.5 mL equivalent to 0.25 mg of betamethasone. Administration way: Oral. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| A1: Etoricoxib / Betamethasone in fixed dose combination tablet. (Laboratorios Silanes S.A. de C.V.) | Drug | Formula: 90 mg/ 0.25 mg. Pharmaceutical Form: Tablet. Dosage: 1 tablet (90 mg/ 0.25 mg) Administration way: oral |
| Measure | Description | Time Frame |
|---|---|---|
| Determine the Cmax. | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the maximum observed concentration following the treatment (Cmax), obtained graphically, from the plasma concentration profile with respect to time. | Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| Determine the AUC 0-t | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the area under the curve from time zero to the last measurable concentration (AUC 0-t) using the linear trapezoidal method. | Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| Determine the AUC 0-inf | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the area under the curve from time zero to infinity calculated (AUC 0-inf). | Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| Determine the Tmax | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the time of the maximum measured concentration (tmax) obtained graphically, from the plasma concentration profile with respect to time. | Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| Determine the Ke | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the elimination rate (Ke), estimated from the terminal linear portion of the plasma concentration profile with respect to time (on a semi-log scale). |
| Measure | Description | Time Frame |
|---|---|---|
| Determine the frequency of occurrence of adverse events | The percentage of frequency of appearance of each adverse event was evaluated. | 1, 15 and 29 days |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Lourdes Garza - Ocañas, Dr. med | Department of Pharmacology and Toxicology of the Faculty of Medicine of the Universidad Autónoma de Nuevo León. | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Department of Pharmacology and Toxicology of the Faculty of Medicine of the Universidad Autónoma de Nuevo León | Monterrey | Nuevo León | 64460 | Mexico |
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| A2: Etoricoxib (Arcoxia®, Laboratorios Schering-Plough, S.A. de C.V.) | Drug | A2: Pharmaceutical Form: Tablet Formula: 90 mg Dosage: 1 tablet of 90 mg Administration way: oral |
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| A3: Betamethasone (Celestone® Pediatric, Laboratorios Schering-Plough, S.A. de C.V.) | Drug | A3: Pharmaceutical Form: Solution Formula: Each 100 mL of solution contains 50 mg of betamethasone. Dosage: 0.5 mL equivalent to 0.25 mg of betamethasone. Administration way: Oral. |
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| Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| Determine the T1/2 | Evaluate the pharmacokinetics profile of the fixed dose Etoricoxib / Betamethasone employing the half time elimination (t1/2) by the quotient of Ln(2) Ke. | Baseline, 0.25, 0.50, 0.75, 1.00, 1.25, 1.50, 2.00, 2.50, 3.00, 4.00, 6.00, 8.00, 12.00, 14.00, 24.00, 36.00, 48.00 and 72.00 hours. |
| ID | Term |
|---|---|
| D001623 | Betamethasone |
| D000077613 | Etoricoxib |
| ID | Term |
|---|---|
| D011246 | Pregnadienetriols |
| D011245 | Pregnadienes |
| D011278 | Pregnanes |
| D013256 | Steroids |
| D000072473 | Fused-Ring Compounds |
| D011083 | Polycyclic Compounds |
| D013259 | Steroids, Fluorinated |
| D013450 | Sulfones |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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