Diclofenac gel

Topical diclofenac gel applied once a day for at least 6 weeks patients complain about discomfort [4]... 

Novakova, L., Solichova, D., and Solich, P. 2006. Advantages of ultra-performance liquid chromatography over high-performance liquid chromatography Comparison of different analytical approaches during analysis of diclofenac gel. J. Sep. Sci. 29 2433-2443. 

Diclofenac gel is indicated for the relief of the pain of osteoarthritis of the joints amenable to topical treatments such as the knees and those of the hands. Diclofenac patch is indicated for the topical treatment of acute pain due to minor strains, sprains and contusions [2,3]. In controlled trials during the premarketing development approximately 600 patients with minor sprains, strains, and contusions were treated safely with diclofenac patch for up to 2 weeks [4j. A randomized, double-blind, placebo-controlled, trial evaluated the efficacy and tolerability of diclofenac patch, self-administered every 12 h to injury site, in 384 patients aged 18-65 years with minor soft tissue injury and moderate to severe pain intensity >5 (0-10 scale). The most common injuries were contusion (42.6%), strain (31.1%), and sprain (24.4%) most common sites were ankle, shoulder, knee, and foot (67.3%). Patients treated with diclofenac patch experienced improved mean pain scores (40.4% of baseline score) vs. patients using placebo (47.4%, P < 0.05) with an overall pain reduction of 14.8% (Figure 52.3). Patients treated with the patch reached pain resolution 3 days sooner than those in the placebo group (median 10.0 vs. 13.5 days, P = 0.01). Patient response to treatment was rated good to excellent 57.8% for the diclofenac patch vs. 48.4% placebo (P < 0.01). 

Both diclofenac gel and the diclofenac patch have been designed with the idea of providing local analgesia... 

Diclofenac is available as dispersible tablets, tablets, gel, suppositories and for intravenous or intramuscular injection. The maximum dose of diclofenac administered via any route is 150 mg. As v/ith other non-steroidal anti-inflammatory drugs, concomitant use in patients receiving venlafaxine increases the risk of bleeding. 

A 0.1% ophthalmic preparation is recommended for prevention of postoperative ophthalmic inflammation and can be used after intraocular lens implantation and strabismus surgery. A topical gel containing 3% diclofenac is effective for solar keratoses. Diclofenac in rectal suppository form can be considered for preemptive analgesia and postoperative nausea. In Europe, diclofenac is also available as an oral mouthwash and for intramuscular administration. 

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). 

Several studies have reported on the enhanced bioavailability of cutaneous drugs using o/w and w/o MEs compared to conventional emulsions, gels or solutions, mesophases, micellar and inverse micellar systems, and vesicles [93], Moreover, a diverse range of drug molecules such as ketoprofen, apomorphine, estradiol, lido-caine [94-97], indomethacin and diclofenac [98], prostaglandin Ei [99], aceclofenac... 

Diclofenac sodium is the active of a variety of different topical, mainly gel, preparations. These preparations are as photosensitive as aqueous solutions, which show a 30% decrease in content after one hour. The absorption of diclofenac up to about 330 nm requires the use of compounds absorbing in the UV region from 300 to 350 nm. 

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. 

Figure 26 Influence of several different excipients on the photostability of diclofenac sodium (1% in hydroxyethylcellulose gel) (Suntest CPS+, window glass filter, 415W/mq. ( ) Without excipients, ( ) unsaturated Sojalecithin (30mg/mL), (O) saturated Sojalecithin (30mg/mL),...

Several NSAIDs have topical preparations, for example ibuprofen (Ibugel), diclofenac (Voltarol emulgel), piroxicam (Feldene gel) and ketoprofen (Oruvail gel). The objective is to produce therapeutic local concentrations without (undesirable) systemic... 

Kerr OA, Kavanagh G, Horn H. Allergic contact dermatitis from topical diclofenac in Solaraze gel. Contact Dermatitis 2002 47(3) 175. 

Included in the FDA Inactive Ingredients Guide (IV infusions, SC implants, and topical preparations). Available in the USA as a 50% solution for irrigation in the treatment of interstitial cystitis. Also available in Canada as a 70% solution for use as a topical antifibrotic and in Germany as a topical gel containing 10% dimethyl sulfoxide for the treatment of musculoskeletal and joint disorders. Included in topical formulations of idoxuridine and diclofenac licensed in the UK. 

In some conditions, the normalized gel layer thickness (=(S — R)/a) may reach a constant value because the synchronization of the swelling and eroding fronts generates pseudo-order release of a solute incorporated in the polymeric matrix. Experimental results concern mixes made of the drug diclofenac sodium and the excipient poly(vinyl alcohol), HPMC type 2208 or NaCMC (Fig. 9). 

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