Pharmacokinetics in the oral cavity: fluoride and other active ingredients

Modern commercial toothpastes contain therapeutic ingredients to combat various oral conditions, for example, caries, gingivitis, calculus and tooth stain. The efficient delivery and retention of such ingredients in the mouth is essential for good performance. The aim of this chapter is to review the literature on the oral pharmacokinetics of, primarily, fluoride but also other active ingredients, mainly anti-plaque agents. Elevated levels of fluoride have been found in saliva, plaque and the oral soft tissues after use of fluoridated toothpaste, which persist at potentially active concentrations for hours. Both experiment and mathematical modelling suggest that the soft tissues are the main oral reservoir for fluoride. Qualitatively similar observations have been made for anti-plaque agents such as triclosan and metal cations, though their oral substantivity is generally greater. Scope for improved retention and subsequent efficacy exists.