Diclofenac sodium and diclofenac potassium in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of 18 rabbits in normal and Escherichia coli induced febrile condition with a washout period of 7 days. Biochemical and physiological parameters were measured in both normal and febrile state. Diclofenac levels in plasma were determined using a reversed-phas...

Diclofenac sodium and alginate was intercalated into montmorillonite to form uniform sized beads by gelation method. The structure and surface morphology of the synthesized composite beads were characterized by powdered X-ray diffraction, Fourier transform infrared spectroscopy, thermo gravimetric analysis and scanning electron microscopy. Diclofenac release kinetics of the composite in simulat...

This study demonstrates the effectiveness of a peptide shuttle in delivering diclofenac into and through human epidermis. Diclofenac was conjugated to a novel phenylalanyl-N-methyl-naphthalenylalanine-derived diketopiperazine (DKP) shuttle and to TAT (a classical cell penetrating peptide), and topically applied to human epidermis in vitro. DKP and TAT effectively permeated into and through huma...

Diclofenac is eliminated predominantly (approximately 50%) as its 4'-hydroxylated metabolite in humans, whereas the acyl glucuronide (AG) pathway appears more important in rats (approximately 50%) and dogs (>80-90%). However, previous studies of diclofenac oxidative metabolism in human liver microsomes (HLMs) have yielded pronounced underprediction of human in vivo clearance. We determined the ...

Pharmaceutical aviailability of diclofenac sodium from solid dispersions of PEG 6000 have been studied in comparison to those of the corresponding physical mixtures and pure diclofenac sodium. The diclofenac sodium is poorly water soluble drug. The properties of diclofenac sodium-PEG 6000 solid dispersions have been determined by the methods of differential scanning calorimetry (DSC), X-ray dif...

BACKGROUND COX-2 inhibitors have an antitumor potential and have been verified by many researchers. Treatment of cancer cells with external stressors such as irradiation can stimulate the over-expression of COX-2 and possibly confer radiation resistance. In this study, we tested if topical diclofenac, which inhibits both COX-1 and COX-2, administration rendered prostate tumor cells sensitize to...

Diclofenac potassium is a widely used non-steroid anti-inflammatory drug which is absorbed more quickly than diclofenac sodium, Reported cases of rhabdomyolisis after only diclofenac are rare, we survey three cases in the literature. . We report a case of a 50 year-old man, chronic smoker and allergic to aspirin who developed a rhabdomyolysis associated with glossopharyngeal edema after oral ad...

Purpose This study was performed to evaluate topical 1% diclofenac/3% menthol gel in treating ankle sprain. Design In this randomized, double-blind, placebo-controlled trial, adolescents and adults with acute ankle sprain (N = 385) applied 4 g of gel containing 1% diclofenac/3% menthol (n = 117), 1% diclofenac (n = 112), 3% menthol (n = 77), or placebo (n = 75) four times daily. The primary out...

Diclofenac belongs to non-steroidal anti-inflammatory drugs (NSAIDs) and non-selective COX inhibitors. The aim of this study was to examine the effect of diclofenac on endothelial cell proliferation under the influence of hypoxia or inflammatory conditions. Another goal was to check whether diclofenac modulates the secretion of angiogenic factors such as VEGF and bFGF in human microvascular end...

The transformed monocyte/macrophage cell line J774.2 undergoes apoptosis when treated for 48 h with competitive inhibitors of cyclooxygenase (COX) isoenzymes 1 and 2. Many of these nonsteroid antiinflammatory drugs (NSAIDs), but in particular diclofenac, induce during this time period a COX activity that coincides with a robust induction of COX-2 protein. Induction of this activity requires hig...