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 characteristics of a bioadhesive buccal slow-release tablet of miconazole has been evaluated. The adhesion time and salivary miconazole levels were measured after application of the tablet to the gingiva, the cheek and the palate in 10 healthy volunteers. The longest adhesion time noted was for the gingiva (565 min), compared to the palate and cheek with 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 clearance 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 miconazole concentrations comparable to those observed with the gingival tablet in healthy volunteers, were obtained after application to the cheek.
Bouckaert
S
S
Laboratory of Pharmaceutical Technology, University of Gent, Belgium.
Lefebvre
R A
RA
Colardyn
F
F
Remon
J P
JP
D000268:Adhesiveness; D000278:Administration, Buccal; D000328:Adult; D000368:Aged; D003128:Coma; D003692:Delayed-Action Preparations; D005260:Female; D005881:Gingiva; D006801:Humans; D007442:Intubation, Intratracheal; D008297:Male; D008825:Miconazole / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008875:Middle Aged; D010159:Palate; D012463:Saliva / Q000378:metabolism; D013607:Tablets
D003692:Delayed-Action Preparations; D013607:Tablets; D008825:Miconazole