Pharmacokinetics and Tolerability of Meloxicam Gel Compared to Meloxicam Tablets in Healthy Subjects

Pharmacokinetics and Tolerability of 2 x 15 mg Meloxicam (2 x 0.3 g Topical Gel) Over 7 Days Compared to 7.5 mg Meloxicam Tablet (Single Oral Dose) in Healthy Subjects. A Two-way Cross-over, Randomized, Open Study

Study to gain information on the percutaneous absorption of meloxicam after administration of a topical gel over 7 days.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Meloxicam tablet; Drug: Meloxicam gel

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy subjects as determined by results of screening
• Signed written informed consent in accordance with Good Clinical Practice and local legislation
• Age >= 18 and <= 50 years
• Broca >= -20% and <= + 20 %

Exclusion Criteria:

• Any findings of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of the gastrointestinal tract (except appendectomy)
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
• Chronic or relevant acute infections
• Hypersensitivity to meloxicam and any of the excipients or non-steroidal antirheumatic agents
• Intake of drugs with a long half-life (>24 hours) (<= 1 month prior to administration or during the trial)
• Use of any drugs which might influence the results of the trial (<= 10 days prior to administration or during the trial)
• Participation in another trial with an investigational drug (<= 2 months prior to administration or during the trial)
• Smoker (> 10 cigarettes or > 3 cigars or >3 pipes/day)
• Inability to refrain from smoking on study days
• Known alcohol abuse
• Known drug abuse
• Blood donation (<= 1 months prior to administration)
• Excessive physical activities (<= 5 days prior to administration)
• History of hemorrhagic diatheses
• History of gastrointestinal ulcer, perforation or bleeding
• History of bronchial asthma
• Any laboratory value outside the normal range of clinical relevance
• History of dermatological diseases
• Skin disease and/or skin lesions at the site of planned application

For female subjects:

• Pregnancy
• Positive pregnancy test
• Breast feeding

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Meloxicam gel	Drug: Meloxicam gel
ACTIVE_COMPARATOR: Meloxicam tablet	Drug: Meloxicam tablet

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Analysis of plasma concentration-time course after topical dose	up to 264 hours after first topical administration
Determination of the ratio AUCss topical/AUC0-∞ oral	up to 96 hours after oral administration

Secondary Outcome Measures

Outcome Measure	Time Frame
Maximum measured concentration of the analyte in plasma (Cmax)	up to 96 hours after oral administration
Time from dosing to the maximum concentration of the analyte in plasma (Tmax)	up to 96 hours after oral administration
Total area under the plasma drug concentration time curve (AUC) from time of administration to the time of the last quantifiable drug concentration (AUC0-t)	up to 96 hours after oral administration
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞)	up to 96 hours after oral administration
Terminal half-life of the analyte in plasma (t½)	up to 96 hours after oral administration
Apparent terminal elimination rate constant	up to 96 hours after oral administration
Apparent clearance of the analyte in plasma following extravascular administration (CL/F)	up to 96 hours after oral administration
Apparent volume of distribution of the analyte during the terminal phase (Vz/F)	up to 96 hours after oral administration
Mean residence time (MRTtot)	up to 96 hours after oral administration
Excretion of metabolites in urine	0-24 hours after oral administration
Predose concentration of the analyte in plasma at steady state immediately before administration of the next dose (Cpre,ss)	up to 264 hours after first topical administration
Minimum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmin,ss)	up to 264 hours after first topical administration
Maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ (Cmax,ss)	up to 264 hours after first topical administration
Total area under the plasma drug concentration time curve (AUC) during a steady state interval (AUCss)	up to 264 hours after first topical administration
Terminal half-life of the analyte in plasma (t½)	up to 264 hours after first topical administration
Apparent terminal elimination rate constant	up to 264 hours after first topical administration
Occurence of adverse events	up to 24 days
Assessment of local and systemic tolerability	up to 24 days

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: September 1, 1998
• Primary Completion (ACTUAL): November 1, 1998

Study Registration Dates

• First Submitted: July 4, 2014
• First Submitted That Met QC Criteria: July 7, 2014
• First Posted (ESTIMATE): July 8, 2014

Study Record Updates

• Last Update Posted (ESTIMATE): July 8, 2014
• Last Update Submitted That Met QC Criteria: July 7, 2014
• Last Verified: July 1, 2014

More Information

Terms related to this study

• 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; Cyclooxygenase 2 Inhibitors; Meloxicam
• Other Study ID Numbers: 107.214