A. Wildfeuer et al., A NEW PHARMACEUTICAL CONCEPT FOR THE TREATMENT OF OROPHARYNGEAL AND ESOPHAGEAL CANDIDOSIS WITH FLUCONAZOLE, Mycoses, 39(9-10), 1996, pp. 357-360
Administration of fluconazole in capsule form has proved effective in
the prophylaxis and treatment of mucosal candidosis, particularly in i
mmunosuppressed patients. An additional topical effect in oropharyngea
l and oesophageal candidosis might be expected with a fluconazole susp
ension. This hypothesis was therefore tested in a crossover study in 1
2 healthy volunteers in whom the concentrations of the antimycotic wer
e measured in saliva and plasma after oral administration of 100 mg fl
uconazole as either a capsule or a suspension. The time courses of the
fluconazole concentrations were very similar with the two formulation
s in plasma, but significantly different in saliva. Thus, the mean C-m
ax for fluconazole in saliva of 551 mu g ml(-1) was reached 5 min afte
r ingestion of the suspension, compared with a value of 3 mu g ml(-1)
some 4 h after taking the capsule. The mean concentration of the antim
ycotic in saliva over the observation period (0-96 h) was more than 80
% higher with the suspension than with the capsule.