Buccal absorption of triclosan following topical mouthrinse application.
OBJECTIVE
To determine clinically the buccal absorption and plaque retention of triclosan from a mouthrinse containing 0.03% triclosan.


METHODS
15 ml of the triclosan oral rinse (N=9) or placebo mouthrinse (N=12) was used twice daily for 21 days in humans. Blood, dental plaque and the expectorated oral rinse were collected prior to, during the treatment period at given intervals, and 8 days after the treatment. Dental plaque and blood samples were collected 1 hr and 4 hr after the morning rinse, respectively. The oral retention of triclosan was calculated by subtracting the amount of triclosan recovered in the expectorate from the triclosan dose applied (4.50 mg) in the mouthrinse. Plasma samples were analyzed for free triclosan (the parent molecule) and its glucuronide and sulfate conjugates, whereas dental plaque was analyzed only for total triclosan.


RESULTS
No significant treatment-related adverse effects were observed during the clinical phase of the study. The average daily oral retention of triclosan was calculated to be 0.660 mg, which is 7.33% of the triclosan dose applied (2 x 4.50 mg). Plaque contained an average 20.5-46.4 microg of triclosan per g of plaque collected. At various sampling times, mean plasma concentrations were: no detectable triclosan, 63.8-86.3 microg/ml of triclosan glucuronide and 8.23-18.0 ng/ml of triclosan sulfate. The mean total triclosan plasma concentration ranged from 74.5 to 94.2 microg/ml with plateau concentrations reached after 2 days of dosing. Eight days after the last treatment the triclosan plasma concentration returned to baseline levels (< 2 ng/ml).
Lin
Y J
YJ
Colgate-Palmolive Company, NJ, USA.
D000042:Absorption; D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000891:Anti-Infective Agents, Local / Q000032:analysis / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D003773:Dental Plaque / Q000737:chemistry / Q000378:metabolism; D005500:Follow-Up Studies; D005881:Gingiva / Q000378:metabolism*; D020719:Glucuronides / Q000097:blood; D006801:Humans; D008297:Male; D009061:Mouth Mucosa / Q000378:metabolism*; D009067:Mouthwashes / Q000032:analysis / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010919:Placebos; D013431:Sulfates / Q000097:blood; D014260:Triclosan / Q000032:analysis / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use
D000891:Anti-Infective Agents, Local; D020719:Glucuronides; D009067:Mouthwashes; D010919:Placebos; D013431:Sulfates; D014260:Triclosan