Diclofenac formulation

Fakeye, TO., A.O. Adegoke, O.C. Omoyeni, and A A. Famakinde. 2007. Effects of water extract of Hibiscus sabdarffa, Linn. (Malvaceae) RoseUe on excretion of a diclofenac formulation. Phytother. Res. 21(l) 96-98. 

Dubey R, Martini LG, and Christie M. (2013). Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with Zolmitriptan and Diclofenac Formulation and in vitro-in vivo characterization. AAPSJ, 16, 214-220. 

Leeson RM, Harrison S, Ernst CC, Hamilton DA, Mermelstein FH, Gawarecki DG, Moshman M, Garr DB. Dyloject ", a novel injectable diclofenac formulation, offers greater safety and efficacy than Voltarol for post-operative dental pain. RegAnesth Pain Med 2007 32 303-310. 

Diclofenac is an exceedingly potent COX inhibitor slightly more efficacious against COX-2 than COX-1. Its absorption from the gastrointestinal tract varies according to the type of pharmaceutical formulation used. The oral bioavailability is only 30-80% due to a first-pass effect. Diclofenac is rapidly metabolised (hydroxylation and conjugation) and has a plasma half-life of 1.5 h. The metabolites are excreted renally and via the bile. 

Zupancic Bozic D, Vrecar F, Kozjek F. Optimization of diclofenac sodium dissolution from sustained release formulations using an artificial neural network. Eur... 

Diclofenac (a non-steroidal anti-inflammatory drug) is marketed as Voltarol oral slow-release formulations. 

Pharmacokinetics The pharmacokinetics following oral administration of a single dose or multiple doses of diclofenac/misoprostol to healthy subjects under fasted conditions are similar to the pharmacokinetics of the 2 individual components. Food decreases the multiple-dose bioavailability profile of both formulations. 

Rheumatoid arthritis - 150 to 200 mg/day in divided doses (50 mg 3 or 4 times/day [diclofenac sodium or potassium] or 75 mg twice/day [diclofenac sodium]). Dosages greater than 225 mg/day of the delayed-release diclofenac sodium formulation and dosages greater than 200 mg/day of immediate-release diclofenac potassium formulation are not recommended. 

Bioactive compounds from Blumea gariepina salicin, salicylic acid, tenoxicam, ketorolac, piroxicam, tolmetin, naproxen, flurbiprofin, diclofenac, and ibuprofen in pharmaceutical formulations and biological samples ... 

Diclofenac sodium, famotidine and ketorolac were analysed utilising their formation of a coloured charge transfer complex with 2,4 dichloro-6-nitrophenol. The complexes were detected by UV/visible spectrophotometry at 450 nm. The method was not affected by the presence of common excipients in the formulations analysed. The precision and accuracy of the method was comparable to that of HPLC methods used to analyse the same samples. ... 

Ruggedness test on a TLC assay of a degradation product of diclofenac sodium in a pharmaceutical formulation [1]... 

A formulation containing an anti-inflammatory agent (diclofenac sodium), two inert matrices (ethylcellulose and polyvinyl chloride), a lubricant (magnesium stearate) and talc was optimized and prepared by a double compression process. 

From a minimum number of experiments, the Hadamard matrix gives the possibility of estimating the mean effects of four parameters. Among them, the particle size range had the most important effect in the release of diclofenac sodium. By interpreting data, a factorial design including only two parameters was applied from which an optimum formulation was found. 

A topical 3% gel formulation of the nonsteroidal anti-inflammatory drug diclofenac (Solaraze) has shown moderate effectiveness in the treatment of actinic keratoses. The mechanism of action is unknown. As with other NSAIDs, anaphylactoid reactions may occur with diclofenac, and it should be given with caution to patients with known aspirin hypersensitivity (see Chapter 36). 

Cevc, G., and G. Blume. 2001. New, highly efficient formulation of diclofenac for the topical, transdermal administration in ultradeformable drug carriers. Transfersomes. Biochim Biophys Acta 1514 191. 

Reer, O., T.K. Block, and B.W. Muller. 1994. In vitro corneal permeability of diclofenac sodium in formulations containing cyclodextrins compared to the commercial product Voltaren Ophtha. J Pharm Sci 83 1345. 

Alpdogan and Sungur [50] developed an indirect atomic absorption spectroscopy method for the determination of mefenamic and flufenamic acids, and diclofenac sodium, based on the complexation with copper (II) amine sulfate. The complex was extracted into chloroform, and the concentrations of substances were determined indirectly by AAS measurement of copper after re-extraction into 0.3 N nitric acid solution. The developed method was applied to the assay of the substances in commercial tablet formulations. The results were statistically compared with those obtained by HPLC method by t- and F tests at 95% confidence level. Calculated t and F values were both lower than the table values. 

A more significant side effect has been reported with topical diclofenac ophthalmic solntion. Keratolysis (corneal melting) was associated with a small nnmber of cases in high-risk patients after ophthalmic snrgery. Responsibility for this side effect has been attribnted subsequently to the vitamin E-based solnbilizer/preserva-tive in the generic formulation, which has been withdrawn from the marketplace. 

Diclofenac sodium 0.1% (Voltaren, Ciba), one of the topical ophthalmic NSAIDs derived from oral formulations. 

Diclofenac sodium is an example where cyclodextrin inclusion has a positive effect on the photostability of the gel formulation. Spray dried diclofenac-cyclodextrin complexes in hydroxyethylcellulose gels showed, after three hours of irradiation. 

Fini, A. Fazio, G. Rabasco, A.M. Fernandez-Hervas, M.J. Holgado, M.A. Pre-formulation study of diclofenac salts, Proc. 14th Pharm. Tech. Congress, Barcelona, Spain,... 

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