Nonionic Bisphenols

Triclosan is a broad-spectrum antimicrobial compound. It was originally used in soaps, antiperspirants, and cosmetic toiletries as a germicide. Today, triclosan is incorporated into toothpaste because of its wide spectrum of antimicrobial activities and low toxicity.

Pharmacokinetics

Triclosan is retained in dental plaque for at least 8 hours, which in addition to its broad antibacterial property could make it suitable for use as an antiplaque agent in oral care preparations. However, the compound is rapidly released from oral tissues, resulting in relatively poor antiplaque properties as assessed in clinical studies of plaque formation. This observation is further corroborated by a poor correlation between minimal inhibitory concentration values generated in vitro and clinical plaque inhibitory properties of triclosan. Improvement of substantivity was accomplished by incorporation of triclosan in a polyvinyl methyl ether maleic acid copolymer (PVM/MA, Gantrez). With the combination of PVM/MA copolymer and triclosan, the substantivity of the triclosan was increased to 12 hours in the oral cavity.

Mechanism of Action

Triclosan is active against a broad range of oral grampositive and gram-negative bacteria. The primary target of its antibacterial activity is the bacterial cell membrane. High concentrations cause membrane leakage and ultimately lysis of the bacterial cell. Effects at lower

TABLE 42.1 Comparison of Antiplaque Agents in Oral Rinses

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