DICLODENT Oromucosal solution (Mouthwash) Ref.[6792] Active ingredients: Diclofenac

Spectrofluoroscopy has shown that diclofenac concentrates in the oral mucosa and then is gradually absorbed, thus producing haematic concentrations that are very low, and insufficient to express pharmacological effects.

Diclofenac is eliminated primarily in the urine, in the form of metabolite, and the remaining part is excreted in the bile and faeces.

Oral diclofenac is rapidly and almost completely absorbed from the gastrointestinal (GI) tract: however, the drug undergoes extensive first-pass metabolism in the liver, with only about 50-60% of a dose as enteric-coated tablets reaching the systemic circulation as unchanged drug.

Following oral administration of a single 25, 50, 75, or 150 mg dose as enteric-coated tablets in healthy adults, average peak plasma diclofenac concentrations of 0.5-1, 1-1.5, 2, and 2.5 mg/mL, respectively within about 1.5-3 hours. The area under the plasma concentration-time curve (AUC) increases linearly with single diclofenac doses of 25-150 mg.

The systemic absorption of mouthwash doses of diclofenac is relatively low compared to oral doses. The systemic bioavailability of diclofenac after 7 days of mouth rinsing b.i.d. with 25 ml of is about 1/10th in terms of AUC and 1/20th to 1/50th in terms of C_max of that obtained with the oral administration of 25 mg diclofenac tablets.

This low absorption should greatly diminish the potential for any systemic drug side-effects when diclofenac is administered by this route.

Three months of oral treatment in rats with a dose of 2 mg/kg/day had produced practically no chronic toxicity. The studies performed showed no mutagenic, carcinogenic or teratogenic effects for diclofenac.