Total and free ketoprofen in serum and synovial fluid after intramuscular injection. 1987

P Netter, and B Bannwarth, and F Lapicque, and J M Harrewyn, and A Frydman, and J N Tamisier, and A Gaucher, and R J Royer
Département de Pharmacologie Clinique, Clinique Rhumatologique, Nancy.

Free and total ketoprofen levels in serum and synovial fluid were determined in 37 patients after a single intramuscular injection of ketoprofen, 100 mg. Free drug was separated by equilibrium dialysis. Ketoprofen was assayed by HPLC. Ketoprofen penetrated into the joints rapidly and significant concentrations were found at 15 minutes. The equilibrium time was about 3 1/2 hours. The AUC for total ketoprofen was greater in serum than in synovial fluid. On the other hand, the free fraction AUC in the serum and synovial fluid were quite similar. The mean residence time in the joint was about three times that in the systemic circulation. Ketoprofen was strongly bound to proteins and the percentage of free ketoprofen was not significantly different between serum and synovial fluid. These results provide a possible explanation for duration of the therapeutic effect of ketoprofen despite the short elimination half-life from the serum.

UI MeSH Term Description Entries
D007273 Injections, Intramuscular Forceful administration into a muscle of liquid medication, nutrient, or other fluid through a hollow needle piercing the muscle and any tissue covering it. Intramuscular Injections,Injection, Intramuscular,Intramuscular Injection
D007660 Ketoprofen An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis. Benzoylhydratropic Acid,19,583 RP,2-(3-Benzoylphenyl)propionic Acid,Alrheumat,Alrheumum,Orudis,Profenid,RP-19583,RP 19583,RP, 19,583,RP19583
D007719 Knee Joint A synovial hinge connection formed between the bones of the FEMUR; TIBIA; and PATELLA. Superior Tibiofibular Joint,Joint, Knee,Joint, Superior Tibiofibular,Knee Joints,Superior Tibiofibular Joints,Tibiofibular Joint, Superior
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D010666 Phenylpropionates Derivatives of 3-phenylpropionic acid, including its salts and esters.
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D004341 Drug Evaluation Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals. Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D005260 Female Females

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