Bioavailability, Pharmacokinetics and Tissue Distribution of R-flurbiprofen Capsules in Healthy Subjects

For previous clinical trials, R-flurbiprofen has been prepared in tablet form. In this study R-flurbiprofen, will be available as gelatine capsules.

This study aims to show the bioavailability of R-flurbiprofen when administered in gelatine capsules. The serum availability will be determined by analysis of pharmakokinetic (pK)-blood samples at different time points. To assess the safety of the administered capsules adverse events will be documented.

Analysis of lipid signaling molecules in plasma will be done to assess the role of this molecules as variable for therapeutic effects.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: R-flurbiprofen

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Frankfurt, Germany, 60528
    • Johann Wolfgang Goethe University Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy subjects aged 18 to 65 years
• Body mass index (BMI) between 18.5 und 30 kg/m2
• Subject is judged to be in good health based on medical history, physical examination, vital sign measurements, and laboratory safety tests
• Subject has no evidence of clinically significant abnormality on echocardiogram (ECG) performed at screening visit and/or prior to administration of the study drug
• Non-Smoker
• Subjects providing informed consent

Exclusion Criteria:

• Subjects with known hypersensitivity to study medication
• Subjects who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs)
• Subjects with a history of peptic ulcer disease and/or gastrointestinal bleeding
• Pregnant women (pregnancy rapid assay required for women with childbearing potential), women currently breast-feeding, or with the intention to breast-feed
• History or evidence of active malignancy within the 24 months prior to entry.
• Subject has a history of fainting during blood draws.
• Subject has had major surgery, donated or lost 1 unit of blood (approximately 500 ml) in the last 4 weeks
• Subject is currently a regular user (including "recreational use) of illicit drugs or has a history of drug (including alcohol) abuse within approximately 2 years.
• Active or history of drug abuse,
• Chronic or acute renal, hepatic or metabolic disorder
• Participation in a clinical study within 30 days prior to screening
• Subjects with immunodeficiencies such as established acquired immunodeficiency syndrome.
• Subject is unable to refrain from or anticipates the use of any medication, (including prescription and non-prescription drugs or herbal remedies (such as St. John's Wort) beginning approximately 2 weeks (or 5 half-lives) prior to administration of the initial dose of study drug until the follow-up visit.
• Subject has a history of any illness that, in the opinion of the study investigator, might confound the results of the study or poses an additional risk to the subject by their participation in the study.
• There is any concern of the investigator regarding the safe participation of the subject in the study or for any other reason, the investigator considers the subject inappropriate for participation in the study.

Study Plan

How is the study designed?

Design Details

• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: R-flurbiprofen; 200 mg R-flurbiprofen in gelatine capsules once	Drug: R-flurbiprofen; 200 mg gelatine capsule once orally; Other Names: Tarenflurbil

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area under the curve (AUC)	assessment of concentration at baseline (0), 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration of study medication	prior to administration, 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration
Time to maximum concentration (Tmax; hours)		prior to administration, 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration
Maximum concentration (Cmax).		prior to administration, 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration
Terminal elimination half-life (t1/2)		prior to administration, 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of volunteers with serious and Non serious adverse events	Number and type of Adverse Events (AEs) and Serious Adverse Events (SAEs) will be documented at V1 (predose and after administration) and at V3 (follow-up visit 8 to 15 days after administration of study medication)	Up to day 15
Analysis of plasma lipid profile	parallel to pK-Analysis plasma lipid profile will be assessed	prior and 30, 60, 90, 120 and 150 minutes and 3, 4, 5, 6, 8, 10, 12 and 24 hours after administration

Collaborators and Investigators

• Sponsor: Gerd Geisslinger
• Collaborators: Fraunhofer Institute for Molecular Biology and Applied Ecology
• Investigators: Principal Investigator: Gerd Geisslinger, Prof MD, Goethe University

Study record dates

Study Major Dates

• Study Start: June 1, 2014
• Primary Completion (Actual): September 1, 2014
• Study Completion (Actual): September 1, 2014

Study Registration Dates

• First Submitted: July 31, 2014
• First Submitted That Met QC Criteria: July 31, 2014
• First Posted (Estimate): August 1, 2014

Study Record Updates

• Last Update Posted (Estimate): September 11, 2015
• Last Update Submitted That Met QC Criteria: September 10, 2015
• Last Verified: September 1, 2015

More Information

Terms related to this study

• Keywords: Pharmakokinetic; capsules; R-Flurbiprofen
• 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; Flurbiprofen
• Other Study ID Numbers: FLIP0112; 2012-001425-27 (EudraCT Number)