Search results for "Aceclofenac"
showing 6 items of 6 documents
Drug metabolism by cultured human hepatocytes: how far are we from the in vivo reality?
2004
The investigation of metabolism is an important milestone in the course of drug development. Drug metabolism is a determinant of drug pharmacokinetics variability in human beings. Fundamental to this are phenotypic differences, as well as genotypic differences, in the expression of the enzymes involved in drug metabolism. Genotypic variability is easy to identify by means of polymerase chain reaction-based or DNA chip-based methods, whereas phenotypic variability requires direct measurement of enzyme activities in liver, or, indirectly, measurement of the rate of metabolism of a given compound in vivo. There is a great deal of phenotypic variability in human beings, only a minor part being…
In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detect…
2001
Objective and Design: The aim of this study was to develop a new, whole-cell test system which is easy to handle and requires a standard equipment for the parallel screening of COX-1 and COX-2 inhibitors.¶Materials: Bovine aortic endothelial cells (BAECs).¶Treatment and methods: Unstimulated bovine aortic coronary endothelial cells (BAECs) were used as a source of COX-1 and BAECs pretreated with ASA (100 μM) and activated with phorbol myristate acetate (PMA) were used as a source of COX-2. The time- and concentration-dependent induction of COX-2 expression in the BAECs was evaluated by a kinetic profile (HPLC analysis) and detected by Western-Blot analysis using polyclonal antibodies agains…
Drug biotransformation by human hepatocytes. In vitro/in vivo metabolism by cells from the same donor.
2001
Abstract Background/Aims : Cultured human hepatocytes are considered a close model to human liver. However, the fact that hepatocytes are placed in a microenvironment that differs from that of the cell in the liver raises the question: to what extent does drug metabolism in vitro reflect that of the liver in vivo? This issue was examined by investigating the in vitro and in vivo metabolism of aceclofenac, an analgesic/anti-inflammatory drug. Methods : Hepatocytes isolated from programmed liver biopsies were incubated with aceclofenac, and the metabolites formed were investigated by HPLC. During the course of clinical recovery, patients were given the drug, and the metabolites, largely prese…
Aceclofenac versus naproxen in the treatment of ankylosing spondylitis: A double-blind, controlled study
1994
Abstract The efficacy and tolerability of aceclofenac and naproxen sodium in the treatment of ankylosing spondylitis (AS) were evaluated and compared in this double-blind, multicenter, controlled study. Of the 130 patients who entered the study, 126 patients met the inclusion criteria. Efficacy was evaluated at baseline, 15 days, and 1, 2, and 3 months using a visual analog scale for spontaneous pain, a zero to three-point scale for pain on movement and pain at rest, and measurements of chest expansion, hand-to-floor distance, Schober's test, and normal daily activities. No significant between-group differences were seen for any of the variables at baseline, except hand-to-floor distance. B…
Aceclofenac cream versus piroxicam cream in the treatment of patients with minor traumas and phlogistic affections of soft tissues: a double-blind st…
1995
Abstract The efficacy and safety of aceclofenac 1.5% cream and piroxicam 1% cream in 220 patients with soft-tissue injuries were evaluated in a double-blind, randomized, multicenter, comparative, parallel-group trial. Patients were randomly assigned to each treatment group to receive therapy three times a day for 7 days. The primary outcome measure of pain was evaluated using a visual analog scale (VAS) at baseline, day 4, and day 7 of the study. Safety was assessed by recording any adverse events that occurred and by monitoring any hemato-biochemical alterations during the study. After days 4 and 7 of treatment, a significant improvement ( P P
Aceclofenac versus piroxicam in the management of osteoarthritis of the knee: A double-blind controlled study
1994
Abstract The objective of this study was to compare the efficacy and tolerability of aceclofenac tablets 100 mg twice daily with piroxicam tablets 20 mg once daily in the treatment of osteoarthritis of the knee or gonarthritis. A randomized, double-blind, controlled study of 3 months' duration was conducted in patients with gonarthritis diagnosed according to the World Health Organization criteria. A total of 212 patients were recruited; 205 patients fully complied with the inclusion-exclusion criteria. Of these, 103 received aceclofenac and 102 received piroxicam. Fourteen patients in the aceclofenac group and 12 patients in the piroxicam group who failed to complete the 3-month treatment …