INFLUENCE OF THE APPLICATION SITE ON BIOADHESION AND SLOW-RELEASE CHARACTERISTICS OF A BIOADHESIVE BUCCAL SLOW-RELEASE TABLET OF MICONAZOLE

The influence of the application site on bioadhesion and release chara cteristics of a bioadhesive buccal slow-release tablet of miconazole h as been evaluated. The adhesion time and salivary miconazole levels we re measured after application of the tablet to the gingiva, the cheek and the palate in 10 healthy volunteers. The longest adhesion time not ed was for the gingiva (565 min), compared to the palate and cheek wit h adhesion times of 210 and 243 min, respectively. Tablets adherent to the palate showed the highest initial salivary drug levels, followed by those adherent to the cheek and gingiva, respectively. The clearanc e rate from the oral cavity was similar when the tablet was applied to the palate and the cheek, but it was markedly decreased when applied to the gingiva. It is concluded that the gingiva is the best site for application of a bioadhesive buccal system for local therapy. A study in 8 comatose intubated patients showed that the application site had to be adapted to the state of the patients treated, as salivary micona zole concentrations comparable to those observed with the gingival tab let in healthy volunteers, were obtained after application to the chee k.