Bioequivalence Study of Nimesulide 100 mg Tablets

Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Study With Single Dosage of Two Oral Preparations Containing Nimesulide 100 mg(Eskaflam®, GlaxoSmithKline México, S.A. de C.V. vs. Mesulid®, Producto de Roche, S.A. de C.V.) in Fasting Healthy Volunteers

The objective of this study was to confirm if two formulations of nimesulide tablets are bioequivalent.

Test product was Eskaflam® (Nimesulide 100 mg tablets; GlaxoSmithKline) and reference product Mesulid® (Nimesulide 100 mg tablets; Syntex for Productos Roche). The single dosage was one tablet.

The study was prospective, open-label, randomized, crossover, single dose, with 02 treatments, 02 sequences and 02 periods, under fasting conditions.

The population was composed of 28 healthy volunteers, both genders, adults between 18-40 years.

The comparative bioavailability of the two formulations was evaluated based in statistical comparisons of relevant pharmacokinetic parameters, obtained from data of drug concentrations in blood.

Study Overview

• Status: Completed
• Conditions: Pain
• Intervention / Treatment: Drug: Nimesulide 100 mg tablets; Drug: Nimesulide 100 mg tablets

• Study Type: Interventional
• Enrollment (Actual): 28
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 36 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

Free will participation according to Mexican regulation, Helsinki Declaration, and Good Clinical Practice.

Healthy, between 18 and 40 years. Body Mass Index between 19 and 27 In good health by complete medical history and laboratory tests. Blood pressure 130-90/ 90-60 mm Hg; heart rate 55-100 beat per minute, respiratory rate 14-20 movements per minute.

Laboratory tests +/- 10% of normal interval (blood cytology, blood chemistry 27 elements, Hepatitis B and C antigens, HIV, urinalysis, anti-doping, pregnancy, electrocardiogram) -

Exclusion Criteria:

Alteration of vital signs Not complying with inclusion criteria History of cardiovascular, kidney, hepatic, muscular, metabolic, gastrointestinal (including constipation), neurologic, endocrine, hematopoietic (any kind of anemia), asthma, mental or organic disease. Those suffering from muscular trauma 21 days before the beginning of the study.

Requirement of any kind of medication during the course of the study, except study medication.

History of dyspepsia, gastritis, esophagitis, duodenal or gastric ulcer. Exposure to medications known as inducers or inhibitors of hepatic enzymes or administration of potentially toxic medication in the 30 days before the study beginning.

Administration of any medication in the 14 days or 5 half-lives (whatever longer) previous to the beginning of the study.

Hospitalization for any cause in the seven months before the beginning of the study.

Administration of investigational drugs in the 60 days before the study. Allergy to any antibiotic or non-steroidal anti-inflammatory analgesic. Alcohol ingestion or intake of beverages containing xanthines (coffee, tea, cocoa, chocolate, mate, cola drinks) or ingestion of charcoal grilled food or grapefruit or orange juice in the 72 hours before the hospitalization or tobacco smoking in the 72 hours before the beginning of the study.

Blood donation or loss => 450 ml in the 60 days before the beginning of the study.

History of drug or alcohol abuse. Positive pregnancy test. Special diet requirement, for instance vegetarian diet. Inability to understand nature, aims, and possible consequences of the study. Evidence of non-cooperative attitude during the study.

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Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: A (reference)/ B (test); initial administration of reference and cross-over to test	Drug: Nimesulide 100 mg tablets; Reference product; Other Names: Mesulid®; Productos Roche SA de CV; Drug: Nimesulide 100 mg tablets; Test product; Other Names: Eskaflam®; GlaxoSmithKline Mexico SA de CV
Experimental: B (test)/ A (reference); initial administration of test and cross-over to reference	Drug: Nimesulide 100 mg tablets; Reference product; Other Names: Mesulid®; Productos Roche SA de CV; Drug: Nimesulide 100 mg tablets; Test product; Other Names: Eskaflam®; GlaxoSmithKline Mexico SA de CV

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Peak Plasma Concentration (CMAX) of nimesulide	Pharmacokinetics	0.0, 0.25, 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, 8.0, 10.0, 12.0, 15.0, 18.0 and 24.0 postdosage
Area under the plasma concentration versus time curve (AUC) of nimesulide	Pharmacokinetics	0.0, 0.25, 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, 8.0, 10.0, 12.0, 15.0, 18.0 and 24.0 postdosage

Collaborators and Investigators

• Sponsor: GlaxoSmithKline

Study record dates

Study Major Dates

• Study Start (Actual): July 18, 2010
• Primary Completion (Actual): July 26, 2010
• Study Completion (Actual): July 26, 2010

Study Registration Dates

• First Submitted: December 6, 2012
• First Submitted That Met QC Criteria: December 6, 2012
• First Posted (Estimate): December 10, 2012

Study Record Updates

• Last Update Posted (Actual): June 12, 2017
• Last Update Submitted That Met QC Criteria: June 9, 2017
• Last Verified: June 1, 2017

More Information

Terms related to this study

• Keywords: Pharmacokinetics; Bioequivalence; Mexico; Nimesulide
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Peripheral Nervous System Agents; Enzyme Inhibitors; Analgesics; Sensory System Agents; Anti-Inflammatory Agents, Non-Steroidal; Analgesics, Non-Narcotic; Anti-Inflammatory Agents; Antirheumatic Agents; Cyclooxygenase Inhibitors; Nimesulide
• Other Study ID Numbers: 117017